PROCESS FOR PRODUCTION OF HIGH PURITY BETA-CAROTENE AND LYCOPENE CRYSTALS FROM FUNGAL BIOMASS

The present invention relates to a simple and economic method of extracting a crystalline Carotenoid compound, such as Beta-carotene, Lycopene, with a purity of at least 99%. The present invention further describes a process to prepare such a highly pure crystalline Carotenoid compound from microbial biomass, using an Anti-purity compound removal process followed by a mono-solvent extraction method. Further the process describes value addition of the co-products recovered during the extraction process thus resulting in a highly economical industrial method for the production of such high purity crystalline Carotenoids compound. 1. A method of extraction of high purity carotenoids from fungal biomass , said method comprising the steps of:a) treatment of carotenoid containing biomass by acidified alcohol;b) separating mechanically the treated biomass from step a) to obtain solid biomassc) extracting the treated biomass (the beta-carotene or lycopene) with an organic solvent;d) filtering the extracted mixture of step c) to recover mother liquor containing carotenoids crystals and the spent biomass;e) repeating the extraction of the spent biomass again with the same solvent;f) filtering the second extracted mixture obtained from the above step to recover mother liquor and the spent biomass;g) recovering pure crystals from the pooled mother liquor obtained from step d) and step f) under chilling conditions by a chilling crystallization method;h) filtering the chilled suspension to get high purity beta-carotene or lycopene crystals; andj) concentrating further the spent mother liquor from step g) with traces of carotenoid to produce oleoresin comprising beta-carotene or lycopene.2. The method of extraction according to wherein the purity of the obtained beta-carotene crystals is 99% or more.3. The method of extraction according to wherein the purity of the obtained lycopene crystals is 99.9%4Blakeslea. The method of extraction according to wherein the fungal biomass used ...

RETINAL DERIVATIVES AND METHODS FOR THE USE THEREOF FOR THE TREATMENT OF VISUAL DISORDERS

Compositions of and methods for using synthetic retinal derivatives as retinoid replacements and opsin agonists are provided. 184-. (canceled)85. A retinyl ester selected from the group consisting of a 9-cis-retinyl ester and an 11-cis-retinyl ester , wherein the ester substituent comprises a carboxylate radical of a Cto Cpolycarboxylic acid , with the proviso that the ester substituent is not tartarate.86. The retinyl ester of claim 85 , which is a 9-cis-retinyl ester of a Cto Cpolycarboxylate.87. The retinyl ester of claim 85 , which is a 9-cis-retinyl ester of a Cto Cpolycarboxylate.88. The retinyl ester of claim 85 , wherein the 9-cis-retinyl ester is 9-cis-retinyl succinate claim 85 , 9-cis-retinyl citrate claim 85 , 9-cis-retinyl ketoglutarate claim 85 , 9-cis-retinyl fumarate claim 85 , 9-cis-retinyl malate or 9-cis-retinyl oxaloacetate.89. The retinyl ester of claim 88 , wherein the 9-cis-retinyl ester is 9-cis-retinyl succinate.90. The retinyl ester of claim 85 , which is an 11-cis-retinyl ester of a Cto Cpolycarboxylate.91. The retinyl ester of claim 85 , which is an 11-cis-retinyl ester of a Cto Ccarboxylate.92. The retinyl ester of claim 90 , wherein the 11-cis-retinyl ester is 11-cis-retinyl succinate claim 90 , 11-cis-retinyl citrate claim 90 , 11-cis-retinyl ketoglutarate claim 90 , 11-cis-retinyl fumarate claim 90 , 11-cis-retinyl malate or 11-cis-retinyl oxaloacetate.93. A pharmaceutical ophthalmological composition claim 90 , comprising:{'sub': 3', '22, 'a synthetic retinyl ester and a pharmaceutically acceptable vehicle, wherein the synthetic retinyl ester is a 9-cis-retinyl ester or an 11-cis-retinyl ester, wherein the ester substituent comprises a carboxylate radical of a Cto Cpolycarboxylic acid.'}94. The pharmaceutical ophthalmological composition of claim 93 , wherein the composition is formulated for local administration to an eye of a human subject.95. The pharmaceutical ophthalmological composition of claim 93 , wherein the composition is ...

Biodegradable compound, lipid particles, composition and kit comprising lipid particles

[Problem] To provide a biodegradable compound having a structure decomposed in a cell, lipid particles containing the compound, and a pharmaceutical composition comprising the lipid particles. [Solution] The compound of the embodiment is represented by the formula (1): P—[X—R—Y—R′-Q] 2 (1). In the formula, P is an alkyleneoxy having an ether bond, X is a divalent linking group having a tertiary amine structure, R is a divalent linking group, R′ is a single bond or a C 1 to C 6 alkylene, and Q is a liposoluble vitamin residue, a sterol residue, or a C 12 to C 22 aliphatic hydrocarbon group. The structure of the compound contains at least one biodegradable group. From the compound in combination with other lipids such as a lipid capable of reducing aggregation, lipid particles can be formed. Further, the compound can be used for a pharmaceutical composition to deliver an activator into cells.

13-Cis-RAMBA RETINAMIDES THAT DEGRADE MNKs FOR TREATING CANCER

The synthesis and in vitro and in vivo anti-breast and anti-prostate cancers activities of novel C-4 heteroaryl 13-cis retinamides that modulate Mnk-eIF4E and AR signaling are discussed. In both breast and prostate cancer cell lines, these compounds induce Mnk1/2 degradation to substantially suppress eIF4E phosphorylation. In prostate cancer cells, the compounds induce degradation of both full-length androgen receptor (fAR) and splice variant AR (AR-V7) to inhibit AR transcriptional activity. The consequences of these multiple activities resulted in inhibition of cell growth and migration and induction of apoptosis. Finally and importantly, the compounds demonstrate strong in vitro and in vivo anti-breast and anti-prostate cancer activities, with no apparent host toxicities. 2. The process as claimed in claim 1 , wherein the process is for the treatment of breast cancer or prostate cancer.3. The process as claimed in claim 2 , wherein R is an imidazole claim 2 , and wherein the compound is selected from the following:Compound 16 in which R′ is the hydrogen, and n is 0;Compound 17 in which R′ is a hydroxyl group in a para-position, and n is 0;Compound 18 in which R′ is a hydroxyl group in an ortho-position, and n is 0;Compound 19 in which R′ is a fluorine in a para-position, and n is 0;Compound 20 in which R′ is a fluorine in a meta-position, and n is 0;Compound 21 in which R′ is the hydrogen, and n is 1;Compound 22 in which R′ is the hydroxyl group in the para-position, and n is 1;Compound 23 in which R′ is the fluorine in the para-position, and n is 1;Compound 24 in which R′ is the fluorine in the meta-position, and n is 1; andCompound 25 in which R′ is the hydroxyl group in the para-position, and n is 2.4. The process as claimed in claim 3 , wherein the compound is selected from the following:Compound 16 in which R′ is the hydrogen, and n is 0;Compound 20 in which R′ is a fluorine in a meta-position, and n is 0; andCompound 22 in which R′ is the hydroxyl group in ...

MANUFACTURE OF CAROTENOID COMPOSITIONS

A extract composition (600) includes capsanthin in the range from 50% to 80%, zeaxanthin in the range from 5% to 15%, and cryptoxanthin the range from 1% to 5%. 1600Capsicum annum. A extract composition () comprising:capsanthin in the range from 50% to 80%;zeaxanthin in the range from 5% to 15%; andcryptoxanthin in the range from 1% to 5%.2. The composition of claim 1 , wherein the capsanthin comprises trans-capsanthin (3R claim 1 ,3″S claim 1 ,5′R)-3 claim 1 ,3′-Dihydroxy-β claim 1 ,κ-caroten-6′-one) claim 1 , the zeaxanthin comprises trans-zeaxanthin (3R claim 1 , 3′R-β claim 1 ,β-carotene-3 claim 1 ,3′-diol) claim 1 , and the cryptoxanthin comprises beta-cryptoxanthin (3R claim 1 ,6′R)-4′ claim 1 ,5′-Didehydro-5′ claim 1 ,6′-dihydro-β claim 1 ,β-caroten-3-ol.3. The composition of claim 1 , wherein the color value of carotenoids ranges from 800 claim 1 ,000 to 1 claim 1 ,250 claim 1 ,000.4. The composition of claim 1 , wherein the composition aids in the management of age related macular degeneration conditions selected from the group consisting of: blurred vision claim 1 , distorted vision claim 1 , reduced central vision claim 1 , and difficulty in adopting low light levels.5. The composition of claim 1 , wherein the composition protects against blue light induced retinopathy by decreasing oxidative and endoplasmic reticulum stress.6. The composition of claim 1 , wherein the composition provides functional and morphological preservation of photoreceptors against blue light damage.7. The composition of claim 1 , wherein the composition lowers intraocular pressure.8. The composition of claim 1 , wherein the composition provides color for a cosmetic selected from the group consisting of: lipstick claim 1 , chap-stick claim 1 , liquid gloss claim 1 , lipstick paste claim 1 , blush claim 1 , lip liner claim 1 , foundation claim 1 , concealer claim 1 , eye contourer claim 1 , eyeliner claim 1 , mascara claim 1 , nail polish claim 1 , eye shadow claim 1 , and body make ...

CRYSTAL FORMS OF ASTAXANTHIN

The invention describes previously undisclosed crystal forms of astaxanthin designated crystal form I and II. It has been surprisingly found that the two crystal forms of astaxanthin show an improved bioavailability, a relatively high solubility in specific organic solvents and an increased long-term stability. For example the new forms are stable in solid form for at least 90 days at a temperature of 20° C.-40° C. It was further found that the two crystal forms can be prepared from each other. Therefore the invention also relates to methods for preparing said crystal forms. In addition, the invention relates to administration forms (hereinafter also called “formulations”) comprising one of the two crystal forms according to the invention or mixtures thereof dissolved or suspended in oil or organic-solvent. 1. A method of preparing an administration form of astaxanthin with improved stability and bioavailability properties , the method comprising incorporating into the administration form at least one crystal form of astaxanthin designated crystal form I and II , whereincrystal form I is characterized by i) An XRPD (X-Ray Powder Diffraction) pattern comprising a peak between 20° and 21°, and ii) A DSC (Differential Scanning Calorimeter) scan showing a phase transition at 225° C.-235° C.; and whereincrystal form II is characterized by i) an XRPD pattern comprising a peak at approximately 11° and 18°, and ii) a DSC scan showing a phase transition at 200° C.-220° C.2. The method according to claim 1 , wherein crystal form I shows a phase transition at 230.8° C.±1.3. The method according to claim 1 , wherein crystal form II shows a phase transition at 210° C.±1.4. The method according to claim 1 , wherein the administration form is stable in solid form for at least 90 days at 20° C.5. An administration form prepared by the method according to claim 1 , wherein the administration form is a fish food comprising at least one of crystal forms I and II.6. An administration ...

Retinoid derivatives with antitumor activity

The present invention relates to compounds of formula (I) and to pharmaceutical compositions containing them: wherein meanings of the substituents are indicated in the description. Such compounds for use in the treatment of cancer and other diseases related to altered angiogenesis, such as arthritic pathology, diabetic retinopathy, psoriasis and chronic inflammatory disease, are also within the scope of the present invention.

ESTERS OF O-SUBSTITUTED HYDROXY CARBOXYLIC ACIDS AND PREPARATIONS THEREOF

Esters of O-substituted hydroxy carboxylic acids are provided having Formula 1, or 2, or both Formulas 1 and 2: 124-. (canceled)26. The ester according to claim 25 , wherein Ris independently selected from the group consisting of substituted and unsubstituted claim 25 , branched- and straight-chain saturated C-Calkyl; substituted and unsubstituted claim 25 , branched- and straight-chain C-Calkenyl; substituted and unsubstituted claim 25 , branched- and straight-chain C-Cdienyl; substituted and unsubstituted claim 25 , branched- and straight-chain C-Ctrienyl; substituted and unsubstituted claim 25 , branched- and straight-chain C-Ctetraenyl; substituted and unsubstituted claim 25 , branched- and straight-chain C-Cpentaenyl; substituted and unsubstituted C-Ccycloalkyl; substituted and unsubstituted C-Ccarbocyclic aryl; substituted and unsubstituted C-Cheterocyclic group; and mixtures thereof.27. The ester according to claim 26 , wherein said alkyl claim 26 , alkenyl claim 26 , dienyl claim 26 , trienyl claim 26 , tetraenyl claim 26 , pentaenyl claim 26 , and cycloalkyl groups are substituted with at least one selected from the group consisting of C-C-alkoxy claim 26 , carboxyl claim 26 , amino claim 26 , C-Caminocarbonyl claim 26 , C-Camido claim 26 , cyano claim 26 , C-C-alkoxycarbonyl claim 26 , C-C-alkanoyloxy claim 26 , hydroxy claim 26 , aryl claim 26 , heteroaryl claim 26 , thiol claim 26 , thioether claim 26 , C-Cdialkylamino claim 26 , C-Ctrialkylammonium and halogen.28. The ester according to claim 26 , wherein said aryl group is at least one selected from the group consisting of phenyl claim 26 , naphthyl claim 26 , anthracenyl claim 26 , and phenyl claim 26 , naphthyl claim 26 , or anthracenyl substituted with one to five substituents.29. The ester according to claim 28 , wherein said one to five substituents of phenyl claim 28 , naphthyl claim 28 , or anthracenyl are selected from the group consisting of C-C-alkyl claim 28 , substituted C-C-alkyl claim 28 ...

RETINOID DOUBLE CONJUGATE COMPOUNDS, COMPOSITIONS THEREOF, AND METHODS FOR TREATING OF SKIN CONDITIONS

Provided are methods of treating certain skin conditions in a human in which the skin of the human in need of such treatment is contacted with an effective amount of a particular composition. 2. The method of claim 1 , wherein the composition further comprises:a carrier; and0.01 to 0.5 wt %, relative to the total weight of the composition, of the molecule of formula Id.3. The method of claim 1 , wherein the composition further comprises:an α-hydroxy acid.6. The method of claim 1 , wherein the molecule of formula (Id) is present in an amount of 0.01 to 0.25 wt %.7. The method of claim 1 , wherein the molecule of formula (Id) is present in an amount of 0.01 to less than 0.2 wt %.8. The method of claim 1 , wherein the molecule of formula (Id) is present in the amount of 0.02 to 0.175 wt %. This is a continuation application of co-pending U.S. application Ser. No. 15/036,467, filed May 13, 2016, which is the U.S. national stage application under 35 U.S.C. § 371 of International Application No. PCT/US2014/065604, filed on Nov. 14, 2014, and claims benefit to U.S. Provisional Application Ser. No. 61/904,532, filed Nov. 15, 2013, the entire disclosures of each of which applications are hereby incorporated by reference herein. The international application was published in English on May 21, 2015, as WO 2015/073769 A1 under PCT Article 21(2).The present invention relates to retinoids, organic acids/alcohols, and alcohols or linked alkyl groups, syntheses and the use of the same in treating skin conditions.Skin is exposed to damage resulting from various sources, including both environmental factors and biochemical processes. Oxidative processes damage proteins, lipids, and other cellular components necessary to maintain the health and appearance of skin, resulting in skin changes, such as skin aging, hyperpigmentation, UV damage, lines, wrinkles, uneven skin texture, etc.Skin aging is accompanied by a number of morphophysiological changes which are described in the ...

METHODS FOR PRODUCING CAROTENOIDS FROM FERMENTATION BY-PRODUCTS

The present technology relates to methods for extracting carotenoids like β-carotene or lutein from oil obtained from/as a by-product derived from a feedstock material like starch-containing material in a processes for producing fermentation products by-products derived from a fermentative production process, in particular from an ethanol fermentation process, wherein the by-product is selected from the group consisting of distillers' wet grain (DWG), distillers' dried grains (DDG), distillers' solubles (DS), distillers' dried solubles (DDS), distillers' dried grain with solubles (DDGS), and mixtures thereof. 1. A method for extracting a carotenoid from oil obtained from a by-product derived from starch-containing material in a processes for producing fermentation products , wherein said method comprises the steps of:a) converting said starch containing material to fermentable sugars;b) fermenting said fermentable sugars with a microorganism;c) separating a by-product from fermentation;d) recovering oil from said by-product;e) contacting said oil with a solid adsorption material;f) separating said solid adsorption material containing said oil; andg) extracting said carotenoid from said adsorption material.2. (canceled)3. The method according to claim 1 , wherein the carotenoid to be extracted is a β-carotene or lutein.4. (canceled)5. The method according to claim 1 , wherein the by-product is selected from the group consisting of distillers' wet grain (DWG) claim 1 , distillers' dried grains (DDG) claim 1 , distillers' solubles (DS) claim 1 , distillers' dried solubles (DDS) claim 1 , distillers' dried grain with solubles (DDGS) claim 1 , and mixtures thereof.6. (canceled)7. The method according to claim 1 , wherein the fermentative production process is an ethanol production process.8. The method according to claim 1 , wherein the starch-containing material is selected from the group consisting of corn claim 1 , wheat claim 1 , barley claim 1 , triticale claim 1 , ...

CAROTENOID DERIVATIVE, PHARMACEUTICALLY ACCEPTABLE SALT THEREOF, OR PHARMACEUTICALLY ACCEPTABLE ESTER OR AMIDE THEREOF

The object of the present invention is to find a carotenoid compound that is excellent in water solubility. 2. The carotenoid derivative according to claim 1 , a pharmaceutically acceptable salt thereof claim 1 , or a pharmaceutically acceptable ester or amide thereof claim 1 ,wherein A in the general formula (a): —CO-A-B-D is a divalent group consisting of 1 to 6 groups of one or more kinds selected from the group consisting of{'sub': 1', '10', '2', '10', '2', '10', '1', '6', '6', '10', '6', '10', '1', '6', 'n', '6', '10', '5', '10, 'sup': 3', '3, '(i) a C-Calkylene group wherein the alkylene group is linear or branched, optionally includes a cyclic alkylene moiety in the chain and optionally has substituent α(s), (ii) a C-Calkenylene group wherein the alkenylene group is linear or branched and optionally has substituent α(s), (iii) a C-Calkynylene group wherein the alkynylene group is linear or branched and optionally has substituent α(s), (iv) —NR— wherein Rrepresents (a1) a hydrogen atom, (b1) a C-Calkyl group, (c1) a C-Caryl group optionally having 1 to 5 substituent β(s) or (d1) a C-Caryl-C-Calkyl group optionally having 1 to 5 substituent β(s) in the aryl moiety, (v) an oxygen atom, (vi) a carbonyl group, (viia) a formula of —S(O)— wherein n represents an integer of 0 or 2, (viii) a C-Cdivalent arylene group optionally having 1 to 4 substituent β(s), (ix) a C-Cdivalent and saturated cyclic hydrocarbon group optionally having 1 to 4 substituent α(s), (x) a divalent and 5- to 7-membered ring heteroarylene group containing 1 to 3 hetero atoms selected from the group consisting of an oxygen atom, a nitrogen atom and a sulfur atom and optionally having 1 to 2 substituent γ(s) and (xi) a divalent and 5- to 7-membered ring saturated heterocyclic group containing 1 to 5 hetero atoms selected from the group consisting of an oxygen atom, a nitrogen atom and a sulfur atom and optionally having 1 to 2 substituent γ(s).'}3. The carotenoid derivative according to claim 1 , ...

METHOD FOR SYNTHESIS OF 9-CIS-BETA-CAROTENE AND FORMULATIONS THEREOF

A formulation includes an active agent, a thickening/solidifying agent, and an antioxidant. The active agent is 9-cis-β-carotene (9CBC) or a derivative thereof of the following formula: 2. The formulation of claim 1 , wherein said thickening/solidifying agent comprises a lecithin or a PEGylated derivative thereof; a lecithin-like substance; a medium chain triglyceride or a mixture thereof; a povidone; a polysorbate; or sorbitol.3. The formulation of claim 2 , wherein said thickening/solidifying agent comprises a lecithin or a PEGylated derivative thereof claim 2 , a lecithin-based product claim 2 , or a povidone.4. The formulation of claim 3 , wherein said lecithin is egg lecithin or soybean lecithin; or said lecithin-based product is L-α-lecithin claim 3 , granular (Acros Organic™) claim 3 , Phospholipon® 50 claim 3 , Phospholipon® 75 claim 3 , Phospholipon® 85G claim 3 , Phospholipon® 90G claim 3 , Phospholipon® 80H claim 3 , Phospholipon® 90H claim 3 , Phospholipon® E25 claim 3 , Phospholipon® E35 claim 3 , Phospholipon® E claim 3 , Phospholipon® LPC20 claim 3 , Phospholipon® LPC25 claim 3 , or Phospholipon® LPC65.5. The formulation of claim 2 , wherein said lecithin-like substance is egg yolk; said medium chain triglyceride is miglyol claim 2 , miglyol 810 claim 2 , or a mixture thereof; or said polysorbate is polysorbate 20 claim 2 , polysorbate 40 claim 2 , polysorbate 60 claim 2 , or polysorbate 80.6. The formulation of claim 1 , wherein said antioxidant is a thiol; a sulphoximine; a metal chelator; sodium bisulfite; sodium metabisulfite; a vitamin; a phenol; a benzoate; uric acid; mannose; propyl gallate; a selenium; a stilbene; a carotenoid; or a mixture thereof.7. The formulation of claim 6 , wherein said thiol is selected from the group consisting of aurothioglucose claim 6 , dihydrolipoic acid claim 6 , propylthiouracil claim 6 , thioredoxin claim 6 , glutathione (GSH) claim 6 , L-cysteine claim 6 , N-acetylcysteine (NAC) claim 6 , cystine claim 6 , ...

1-((3s,4r)-4-(3-fluorophenyl)-1-(2-methoxyethyl)pyrrolidin-3-yl)-3-(4-methyl-3-(2-methylpyrimidin-5-yl)-1-phenyl-1h-pyrazol-5-yl)urea as a trka kinase inhibitor

Provided is Compound (I) or a pharmaceutically acceptable salt thereof, which is an inhibitor of TrkA kinase and is useful in the treatment of diseases which can be treated with a TrkA kinase inhibitor such as pain, cancer, inflammation and inflammatory diseases, neurodegenerative diseases, certain infectious diseases, Sjogren's syndrome, endometriosis, diabetic peripheral neuropathy, prostatitis, pelvic pain syndrome, diseases related to an imbalance of the regulation of bone remodeling, and diseases resulting from Connective Tissue Growth Factor aberrant signaling.

METHOD FOR EXTRACTING USEFUL SUBSTANCES FROM SHRIMP SHELLS

Disclosed is a method for extracting useful substances from shrimp shells. The method comprises: crushing the shrimp shells, mixing the crushed shrimp shells and water, then heating same to 28° C.-35° C., adjusting the pH value to 6.8-7.5, preferably 6.8-7, then adding an alkaline protease and mixing same, heating same to 42° C.-48° C., performing constant-temperature enzymolysis for 50-70 min, and performing sieving to obtain an enzymatic hydrolysate and solid residues; performing centrifugal separation treatment on the enzymatic hydrolysate to obtain a shrimp protein deposit containing astaxanthin; mixing the shrimp protein deposit and water, performing heating while stirring, adjusting the pH value to 6.8-7.0, performing heating to 58° C.-60° C., adding vegetable oil, and performing emulsification for 50-70 min under stirring to obtain an emulsion; and performing centrifugation on the emulsion, and performing delamination to obtain astaxanthin-containing oil in an upper layer, water in a middle layer, and a shrimp protein in a lower layer. The method of the present invention uses waste biomass obtained after shrimps processed as a raw material, and can simultaneously extract several high-value substances, thereby not only improving the utilization rate of the raw material, but also shortening the production cycle; and no organic solvent is added, such that the method is clean, green and environmentally friendly.

Method for producing carotenoid composition

The present invention provides an efficient method for industrially producing a naturally-derived carotenoid composition with a large amount of a carotenoid such as astaxanthin from a culture of a yeast of the genus Xanthophyllomyces without requiring any special extraction equipment and any complicated refinement process and without any need for organic solvents harmful to humans. Provided is a method for producing a carotenoid composition, including the steps of washing a carotenoid-containing yeast of the genus Xanthophyllomyces with an organic solvent (A) at 30° C. or lower, and extracting a carotenoid from the washed yeast with an organic solvent (B) at 10° C. to 70° C.

PROCESS FOR SEPARATING ASTAXANTHAN

Disclosed is a chromatographic process complex for the refining of krill oil extract including desalting, removal of impurities such as trimethylamine oxide (TMAO), and the production of krill oil products including desalted krill oil extract, polar lipid products having polar lipid contents greater than 50 wt-% on a dry or solvent free basis, neutral lipid streams for biodiesel production and astaxanthin. The refinery includes a continuous desalting zone, a fixed bed polar lipid extraction zone to adsorb neutral lipids and astaxanthin to provide a polar lipid extract stream comprising solvent and polar lipids and being essentially free of neutral lipids and astaxanthin, and an astaxanthin separation zone to recover essentially pure astaxanthin and provide a neutral lipid stream. The enriched products of the krill oil refinery are essentially free of TMAO and salt and provide products which can be used as dietary supplements and as medicinal additives. 1. A process for separating astaxanthin from a mixture comprising neutral lipids and astaxanthin , said process comprising;e) diluting the mixture in a solvent comprising ethanol and water having an ethanol:water ratio of between of about 95:5 to 99:1 to concentration of about 5 percent by weight of said mixture to provide a diluted astaxanthin mixture;f) introducing the diluted astaxanthin mixture to an astaxanthin extraction zone and therein contacting a steam activated carbon adsorbent to adsorb astaxanthin and to provide a neutral lipid rich stream comprising solvent and neutral lipids;g) washing the steam activated carbon adsorbent with heptane to remove the neutral lipids from the steam activated carbon adsorbent;h) regenerating the steam activated carbon with anisole to desorb the astaxanthin to provide an astaxanthin rich stream comprising anisole and astaxanthin;i) recovering the anisole from the astaxanthin rich stream to provide an astaxanthin product; and,j) returning at least a portion of the anisole to ...

NEW INTERMEDIATES FOR THE VITAMIN A AND beta-CAROTENE SYNTHESIS

The present invention relates to compounds of formula (I) wherein R 1 signifies a C 1 -C 15 alkyl moiety or a C 2 to C 18 alkenyl moiety, to their process of production as well as to their use in organic synthesis, especially as intermediates (building blocks) in the synthesis of vitamin A or β-carotene or derivatives thereof, or other carotenoids, e.g. canthaxanthin, astaxanthin or zeaxanthin, preferably vitamin A.

PROCESSES FOR THE PREPARATION OF UNSATURATED MALONATES

Disclosed is a process for preparing unsaturated malonates and/or their isomers. The process includes the step of reacting an aldehyde and a dialkyl malonate in the presence of a Lewis acid and a carboxylic acid thereby forming an unsaturated malonate. 2. The process of claim 1 , wherein the reaction is performed in the presence of an aprotic dipolar solvent.3. The process of claim 1 , wherein the Lewis acid is a compound of formula MX claim 1 , in which M is a metal selected from group IA or IIA; X is a halogen; and n is 1-4.4. The process of claim 1 , wherein the carboxylic acid is selected from the group consisting of formic acid claim 1 , acetic acid claim 1 , propionic acid claim 1 , citric acid claim 1 , and any combinations thereof.5. The process of claim 2 , wherein the aprotic dipolar solvent is selected from the group consisting of N claim 2 ,N-dimethylformamide (DMF) claim 2 , N claim 2 ,N-dimethylacetamide (DMAC) claim 2 , N-Methyl-2-pyrrolidone (NMP) claim 2 , dimethylsulfoxide (DMSO) claim 2 , and any combinations thereof.6. The process of claim 1 , wherein the reaction is performed at a temperature of 100 to 160° C. for at least 5 hours.8. The process of claim 7 , further comprising the step of converting the compound of formula C or the compound of formula D under an alkoxydecarbonylating condition thereby forming a compound of formula E claim 7 , a compound of formula F claim 7 , or any isomer thereof.10. The process of claim 1 , wherein the dialkyl malonate of formula B is dimethyl malonate or diethyl malonate and the Lewis acid is magnesium chloride.13. The process of claim 12 , further comprising the step of converting Compound I or V to Compound IV.15. The process of claim 1 , wherein the reaction is performed in a batch reactor or a continuous reactor claim 1 , in which the continuous reactor is a single Continuous Stirred Tank Reactor (CSTR) claim 1 , multiple CSTRs in series claim 1 , or a microreactor. This application claims priority to U.S ...

FREE RADICAL- AND REACTIVE OXYGEN SPECIES-REACTING COMPOUNDS

Provided are compounds that generate a peroxide when they react with ozone in the presence of water. Additionally, alkyne compounds reactive with a free radical, a reactive oxygen species (ROS) or another reactive species are provided. Also provided are enol ether, enamine, and vinal thioester compounds reactive with a free radical, a strong acid, a reactive oxygen species (ROS) or another reactive species. Additionally provided are compounds reactive with a free radical, an ROS or another reactive species. The compounds comprise a conjugated moiety operably joined to an alkene moiety and a resonance-transmitting moiety, wherein the resonance-transmitting moiety transmits an electron through the conjugated moiety to the alkene moiety, which reacts with the free radical, an ROS or another reactive species. Also provided are methods of decomposing a free radical, an ROS or another reactive species. The methods comprise contacting the free radical or ROS with any of the above compounds. Also provided are methods of using any of the compounds described herein, and compositions comprising those compounds. Additionally provided are methods of producing the above compounds. 2. The compound of claim 1 , wherein the peroxide is hydrogen peroxide claim 1 , an organic peroxide claim 1 , an organic hydroperoxide claim 1 , a peracid claim 1 , a peroxide ion claim 1 , superoxide claim 1 , benzoyl peroxide claim 1 , performic acid claim 1 , peracetic acid claim 1 , meta-chloroperoxybenzoid acid claim 1 , peroxybenzoic acid claim 1 , a peroxy acid claim 1 , or R—O—O—R.3. The compound of claim 1 , wherein the compound is a monomer.4. The compound of claim 3 , wherein the monomer is less than 1000 MW.5. The compound of claim 1 , wherein the compound is a polymer.69-. (canceled)11. (canceled)13. (canceled)14. The compound of claim 1 , wherein the compound is formulated as a skin treatment composition or as a coating.15. (canceled)16. A method of generating a peroxide claim 1 , the ...

METHOD OF EXTRACTING LUTEIN/XANTHOPHYLLS FROM NATURAL MATERIALS AND HIGHLY PURIFIED LUTEIN/XANTHOPHYLLS OBTAINED FROM THE METHOD THEREOF

The present invention provides the new method for extracting lutein from natural materials wherein the said method comprises of modification of natural lutein ester in the natural materials to free lutein and/or low molecular weight lutein ester, extraction of the said natural materials with supercritical fluid at the optimal conditions. The said method yields high amount of crude lutein with high purity due to the mild condition used for extraction. Therefore, no degradation of the desired product is occurred. The crude lutein can be further purified with chromatography in order to obtain the highly purified lutein. The method according to this invention can be applied to the extraction of xanthophylls or others beside lutein. 1. Method of extracting lutein from natural materials , the method comprising:a. Pretreatment of natural materials containing lutein by modification of natural lutein ester in the natural materials to free lutein and/or low molecular weight lutein ester, which facilitate the extraction process;{'b': 30', '100', '200', '450, 'b. Extraction comprising contacting the pretreated natural materials in (a) with a supercritical fluid, adjusting temperature and/or pressure by selecting optimal conditions between - C, - bar for a certain period of time to allow maximum solubility of the free lutein and/or the low molecular weight lutein ester in the supercritical fluid;'}c. Separation of solid materials from the supercritical fluid, after extraction, adjusting temperature and/or pressure to minimize solubility of extracted materials in the supercritical fluid, and collecting of the extracted materials wherein the extracted materials comprise crude lutein.2. Method according to wherein the natural materials are selected from marigold flower claim 1 , kale claim 1 , spinach claim 1 , algae claim 1 , microbial cells including bacteria claim 1 , yeasts claim 1 , fungi and microalgae or a combination thereof.3. Method according or wherein the natural ...

PROCESS FOR ISOLATING A CAROTENOID FROM A CAROTENOID-PRODUCING BIOORGANISM

The present invention relates to an improved process for isolating a carotenoid from a carotenoid-producing bioorganism, as well as to a formulation comprising such a carotenoid, and the use of such a solid formulation in feed products (or pre-mixes). 1. A process for the isolation of a carotenoid from a carotenoid-producing bioorganism comprising the following steps(i) extraction of the carotenoid from the biomass by at least one solvent (I), and(ii) optionally at least one washing step using at least one solvent (II), which is not miscible with the solvent (I), and(iii) optionally drying the obtained solution which comprises the carotenoid,characterised in that after the step (i) at least one washing step using an aqueous solution of a Brønsted acid is carried out (step (i′)).2. Process according to claim 1 , wherein the Brønsted acid is chosen from the group consisting of phosphoric acid and organic acids.3. Process according to claim 1 , wherein the Brønsted acid is chosen from the group consisting of citric acid claim 1 , tartaric acid and maleic acid.4. Process according to claim 1 , wherein the concentration of the aqueous solution of the Brønsted acid between 0.5-10 weight-% (wt-%) claim 1 , based on the total weight of the aqueous solution.5. Process according to claim 1 , wherein the process is carried out batchwise or continuously.6. Process according to claim 1 , wherein the extraction (step (i)) is usually carried out at a temperature below the boiling point of the solvent.7. Process according to claim 1 , wherein the extraction of the carotenoid from the biomass is carried out in at least one water immiscible solvent.8. Process according to claim 7 , wherein the extraction of the carotenoid from the biomass is carried out in at least one solvent chosen from the group consisting of CHCl claim 7 , chloroform claim 7 , n-heptane and n-hexane.9. Process according to claim 1 , wherein at least washing steps (step (ii)) is carried out after step (i) and ...

METHOD FOR PRODUCING N-RETINOYLCYSTEIC ACID ALKYL ESTER

A method for producing derivatives of N-retinoylaminoalkane sulfonic acid, the method comprising providing retinoic acid, chloroformate, aminoalkanesulfonic acid selected from the group consisting of cysteic acid and alkyl ester thereof, cysteinesulfinic acid and alkyl ester thereof, homocysteic acid and alkyl ester thereof, homocysteinesulfinic acid and alkyl esters thereof, taurine and derivatives thereof, and an organic solvent, and a base, mixing said components under substantial absence of oxidizing compounds thereby forming a reaction mixture comprising a liquid phase, wherein the liquid phase is one phase and the derivatives of N-retinoylaminoalkane sulfonic acid are formed in said liquid phase. 1. A method for producing derivatives of N-retinoylaminoalkane sulfonic acid , the method comprising providing retinoic acid , chloroformate , aminoalkanesulfonic acid selected from the group consisting of cysteic acid and alkyl ester thereof , cysteinesulfinic acid and alkyl ester thereof , homocysteic acid and alkyl ester thereof , homocysteinesulfinic acid and alkyl esters thereof , taurine and derivatives thereof , and an organic solvent , and a base , mixing said components under substantial absence of oxidizing compounds thereby forming a reaction mixture comprising at least a liquid phase , wherein the liquid phase is one phase and the derivatives of N-retinoylaminoalkane sulfonic acid are formed in said liquid phase.2. The method according to claim 1 , wherein the derivatives of N-retinoylaminoalkane sulfonic acid are selected from N-(13-cis-retinoyl)-cysteic acid alkyl ester and N-(all-trans-retinoyl)-cysteic acid alkyl ester claim 1 , the retinoic acid is selected from 13-cis-retinoic acid or all-trans-retinoic acid claim 1 , and the aminoalkane sulfonic acid selected from cysteic acid alkyl ester.3. The method according to claim 1 , wherein the derivatives of N-retinoylaminoalkane sulfonic acid are selected from the sodium salts of N-(13-cis-retinoyl)- ...

Compounds for the treatment of hiv

The invention provides compounds of formula (I): or a salt thereof as described herein. The invention also provides pharmaceutical compositions comprising a compound of formula (I), processes for preparing compounds of formula (I), intermediates useful for preparing compounds of formula I and therapeutic methods for treating a Retroviridae viral infection including an infection caused by the HIV virus.

Method for preparing iodine-doped tio2 nano-catalyst and use thereof in heterogeneously catalyzing configuration transformation of trans-carotenoids

The present invention relates to a method for preparing an iodine-doped TiO 2 nano-catalyst and use of the catalyst in heterogeneously catalyzing configuration transformation of trans-carotenoids. The iodine-doped TiO 2 nano-catalyst is prepared by a sol-gel process using a titanate ester as a precursor and an iodine-containing compound as a dopant in the presence of a diluent, inhibitor and complexing agent. The catalyst exhibits high activity for isomerization of the trans-carotenoids into their cis-isomers within a short catalytic time. The catalyst can be easily prepared and is highly efficient, economical, recyclable and environmentally friendly.

METHOD FOR PREPARING WATER-SOLUBLE ASTAXANTHIN COMPLEX AND AQUEOUS SOLUTION OF ASTAXANTHIN PREPARED THEREBY

Provided is a method for preparing water-soluble astaxanthin complex. The method includes mixing a raw material containing astaxanthin with a solution containing an organic acid and performing cell disruption and leaching and can enable natural astaxanthin to interact with components such as proteins, nucleic acids, or polysaccharides that naturally exist in the raw material, so as to directly prepare water-soluble astaxanthin complex without modifying astaxanthin. The method requires a natural source of astaxanthin, has low equipment requirements and production costs, is simple to operate, green and safe with no organic solvent residues, and easy to industrialize. 1. A method for preparing water-soluble astaxanthin complex , comprising:(1) mixing a raw material containing astaxanthin with a solution containing an organic acid and performing cell disruption to obtain a leachate; and(2) stirring and leaching the leachate in step (1) and performing solid-liquid separation to obtain water-soluble astaxanthin complex.2chlorella. The method according to claim 1 , wherein the raw material containing astaxanthin comprises any one selected from the group consisting of Haematococcus pluvialis claim 1 , Phaffia rhodozyma claim 1 , crustaceans claim 1 , claim 1 , and a combination of at least two selected therefrom.3. The method according to claim 1 , wherein the organic acid in the solution containing an organic acid in step (1) has a mass concentration of 0.1 to 2.0 moL/L.4. The method according to claim 1 , wherein the solution containing an organic acid has a pH of 3.0 to 6.5 claim 1 , preferably 5.0 to 6.3.5. The method according to claim 1 , wherein the organic acid comprises any one selected from the group consisting of malic acid claim 1 , tartaric acid claim 1 , glycine claim 1 , oxalic acid claim 1 , citric acid claim 1 , and a combination of at least two selected therefrom.6. The method according to claim 1 , wherein the solution containing an organic acid is a pH ...

COMPOSITION CONTAINING LUTEIN/LUTEIN ESTER AND APPLICATIONS THEREOF

Disclosed in the present invention are a composition containing lutein/lutein ester and applications thereof. Components of the composition containing lutein/lutein ester comprise lutein/lutein ester, β-carotene and a pharmaceutically acceptable carrier. The weight ratio of lutein/lutein ester to β-carotene is 1:0.1-100. In the present invention, by cooperatively using lutein/lutein ester and β-carotene and using auxiliary natural healthy ingredients, the dosage form of an orally disintegrating tablet is prepared. The orally disintegrating tablet is absorbed through the oral cavity, has fast effectiveness and small first-pass effect, reduces damage of gastric acid to lutein/lutein ester, has high bioavailability, and has the characteristics of nutritional and health-care effects, good mouthfeel and fast absorption. By eating the product, visual power can be obviously enhanced, the ocular blood flow is increased, and eye muscle fatigue is alleviated, and accordingly the morbidities of cataract, senile niacula lutea retinae lesion and adolescent myopia are reduced. 17-. (canceled)10. The composition containing lutein/lutein ester according to claim 8 , whereinthe acidity regulator is one or more selected from the group consisting of citric acid, malic acid, fumaric acid, lactic acid and tartaric acid;the loose agent is one or more selected from the group consisting of soda, baking soda, calcium carbonate and magnesium carbonate;the sugar powder is one or more selected from the group consisting of white granulated sugar powder, fructose powder and glucose powder;the fruit powder is one or more of the darker fruit powders selected from the group consisting of blueberry powder, black currant powder, cranberry powder, tomato powder, grape powder and mulberry powder;the alditol is one or more selected from the group consisting of sorbitol, mannitol, xylitol, and erythritol.11. A method for treating ocular diseases or for providing ocular health care claim 8 , comprising ...

STEREOSELECTIVE SYNTHESIS OF 9-CIS.13,14-DIHYDRORETINOIC ACID AND ITS ETHYL ESTERS

The retinoid X receptors (RXRs) are ligand-activated transcription factors heterodimerize with a number of nuclear hormone receptors, thereby controlling a variety of physiological processes. The invention relates to novel enantiomer compounds which are derivatives of dihydroretinoic acid, their stereoselective synthesis, to pharmaceutical compositions containing the same and to the use of same in the treatment of diseases. 4. An enantiomer compound of 9-cis-13 ,14-dihydroretinoic acid or an ester precursor thereofwherein said compound is selected from the group consisting of(R)-9-cis-13,14-dihydroretinoic acid,(S)-9-cis-13,14-dihydroretinoic acid(9Z,13R)-ethyl-13,14-dihydroretinoate((R)-4) and(9Z,13R)-ethyl 13,14-dihydroretinoate ((S)-4), andsolvates, solid forms and, if appropriate, salts thereof.5. The compound of selected from the group consisting of(R)-9-cis-13,14-dihydroretinoic acid,(S)-9-cis-13,14-dihydroretinoic acid, andsolvates, solid forms and salts thereof.6. The compound of selected from (R)-9-cis-13 claim 4 ,14-dihydroretinoic acid or a solvate claim 4 , solid form or salt thereof.7. A pharmaceutical composition comprising an enantiomerically pure compound selected from the enantiomer compounds according to claim 4 , solvates claim 4 , solid forms and claim 4 , if appropriate claim 4 , salts thereof claim 4 ,in a pharmaceutically acceptable carrier.8. The pharmaceutical composition of comprising an enantiomerically pure compound of 9-cis-13 claim 7 ,14-dihydroretinoic acid claim 7 ,wherein said compound is selected from the group consisting of(R)-9-cis-13,14-dihydroretinoic acid,(S)-9-cis-13,14-dihydroretinoic acid.solvates, salts and solid forms thereof,in a pharmaceutically acceptable carrier.9. The compound of claim 5 ,wherein said compound is selected from the group consisting of(R)-9-cis-13,14-dihydroretinoic acid,(S)-9-cis-13,14-dihydroretinoic acidor a pharmaceutical composition comprising said compound,for use in a therapeutic method.10. The ...

Retinal derivatives and methods for the use thereof for the treatment of visual disorders

Compositions of and methods for using synthetic retinal derivatives as retinoid replacements and opsin agonists are provided.

TRANSESTERIFICATION PROCESS OF RETINOL ESTERS

The present invention relates to a transesterification process of specific compounds comprising isoprenoid units. 2. Transesterification process according to claim 1 , wherein Ris CH claim 1 , —CHand/or —CH claim 1 , preferably —CH3. Transesterification process according to claim 1 , wherein Ris —CH.4. Transesterification process according to claim 1 , wherein the alkali hydroxide is Ca(OH) claim 1 , CsOH claim 1 , KOH and/or NaOH claim 1 , preferably KOH and/or NaOH.5. Transesterification process according to claim 1 , wherein the alcohol is chosen methanol claim 1 , ethanol claim 1 , isopropanol and/or tert-butanol.6. Transesterification process according to claim 1 , wherein the alcohol is methanol.7. Transesterification process according to claim 1 , wherein ratio of the least one alkali hydroxide to the least one alcohol goes from 1:2 to 1:10 claim 1 , preferably from 1:3 to 1:6.8. Transesterification process according to claim 1 , wherein the transesterification is carried out at a temperature between 20° C. and 80° C. claim 1 , more preferably between 30° C. and 70° C.9. Transesterification process according to claim 1 , wherein the transesterification is carried out under reduced pressure.10. Transesterification process according to claim 9 , wherein the pressure goes from 100 to 15000 Pa claim 9 , preferably from 100 to 5000 Pa.11. Transesterification process according to claim 1 , wherein the low boiling side products are removed after or even during the transesterification reaction. The present invention relates to a transesterification process of specific compounds comprising isoprenoid units.Transesterification processes of compounds comprising isoprenoid units are usually carried out by using chloride acids, such as described by Soukup et al. in Tetrahedron Letters Vol. 32 (33), p. 4117-4118, 1991.In view of the ecological problems of halogenides (waste issues), it is desirable to avoid such compounds.But nevertheless an alternative process should be ...

Vitamin Cationic Lipids

Disclosed are cationic lipids comprising a vitamin substructure and an ionizable nitrogen-containing group. Cationic lipids provided herein can be useful for delivery and expression of mRNA and encoded protein, e.g., as a component of liposomal delivery vehicle, and accordingly can be useful for treating various diseases, disorders and conditions, such as those associated with deficiency of one or more proteins. 1. A liposome encapsulating an mRNA encoding a peptide or polypeptide , wherein the liposome comprisesone or more cationic lipids, andoptionally one or more non-cationic lipids, optionally one or more cholesterol-based lipids and optionally one or more PEG-modified lipids; and{'sup': 1', '1, 'wherein the liposome comprises at least one cationic lipid that comprises the structure of Vitamin A, D, E, or K, and also comprises a moiety X, wherein Xis an ionizable nitrogen-containing group.'}13. The liposome of any one of - , wherein Xis O.14. The liposome of any one of - , wherein Ris C-C-alkylene.15. The liposome of any one of - , wherein Ris C-C-alkylene.16. The liposome of claim 14 , wherein Ris unsubstituted C-C-alkylene.17. The liposome of claim 15 , wherein Ris unsubstituted C-C-alkylene.18. The liposome of any one of - claim 15 , wherein Ris —CH— claim 15 , —CH— claim 15 , —CH— claim 15 , —CH— claim 15 , —CH— claim 15 , —CH— claim 15 , —CH— claim 15 , —CH— claim 15 , —CH— claim 15 , —CH— claim 15 , —CH— claim 15 , —CH— claim 15 , —CH— claim 15 , —CH— claim 15 , —CH— claim 15 , —CH— claim 15 , —CH— claim 15 , —CH— claim 15 , —CH— claim 15 , or —CH—.19. The liposome of any one of - claim 15 , wherein Ris —CH— claim 15 , —CH— claim 15 , or CH—.20. The liposome of claim 14 , wherein Ris substituted C-C-alkylene with one or substituents selected from halogen claim 14 , hydroxyl claim 14 , amino claim 14 , thiol claim 14 , ester claim 14 , and thioester.21. The liposome of any one of - claim 14 , wherein Ris C-C-alkenylene or C-C-alkenylene.22. The liposome of ...

Gel composition, method for manufacturing the gel composition, and method for manufacturing an ophthalmic lens using the gel composition

A gel composition comprises hydrophilic monomers, a cross-linking agent, an initiator, and astaxanthin-modified cyclodextrin complexes. The astaxanthin-modified cyclodextrin complexes comprise astaxanthin and modified cyclodextrin. The modified cyclodextrin has a chemical structure of with a hollow cavity, wherein R represents a chemical group having carbon-carbon double bond. The astaxanthin is embedded in the hollow cavity. The disclosure also provides a method for manufacturing a gel composition, and a method for manufacturing an ophthalmic lens using the gel composition.

2-(ALKOXY OR ARYLOXY CARBONYL)-4-METHYL-6-(2,6,6-TRIMETHYLCYCLOHEX-1- ENYL)HEX-2-ENOIC ACID COMPOUNDS, ITS PREPARATION AND USE

Compounds of the formula 1 2. A compound according to wherein R is hydrogen claim 1 , methyl or ethyl.4. The method according to wherein the organocatalyst is selected from the group consisting of ammonium salts of carboxylic acids claim 3 , ammonium salts of polycarboxylic acids claim 3 , and amine components selected from the group consisting of ammonia claim 3 , primary amines claim 3 , secondary amines claim 3 , polyamines claim 3 , amino acids and peptides.5. The method according to wherein the solvent or solvent system forms an azeotrope with water claim 3 , which is constantly removed from the reaction mixture by distillation.6. The method according to wherein the condensation reaction is carried out at about 60-95° C.7. The method according to wherein the solvents are selected from cyclohexane claim 3 , benzene claim 3 , toluene claim 3 , iso-propanol and tert-butanol.9. The method according to wherein the decarboxylation is carried out in a polar aprotic solvent at 75-85° C.10. The method according to wherein the compound of formula 1 is thermally decarboxylated at a temperature of 50-350° C. under flow conditions.12. The method according to wherein the metal salt is LiCl and/or MgCland the solvent is NMP.14. An ester of the formula 4 obtained from the compound of formula 1 according to the method of .15. An acid of the formula 6 obtained from the compound of formula 1 claim 11 , according to the method of .16. A compound of the formula 2 obtained from the compound of formula 1 according to the method of .18. A compound of formula 2 obtained from the compound of formula 1 according to the method of . The invention is concerned with organic compounds their preparation and use as intermediates in the synthesis or fragrance ingredients.Many fragrance ingredients that are used by perfumers in the creation of new and exciting fragrance accords are commodity ingredients, that is, they are non-proprietary and versions of the ingredients, which may differ in price ...

A method for preparing lutein feed additive

The present invention discloses a method for preparing controlled release type lutein feed additive. Steps: lutein extract, glycerol and fat are mixed and dissolved, then alkali liquor is dropped under condition of mechanical stirring and sheering emulsification to allow the lutein to be fully saponified. Then fat is added and alkaline saponification is conducted, adjusting the viscosity and neutralizing and conducting spray granulation to the mixed liquor to obtain controlled release lutein feed additive. By utilizing the combined effects of glycerol and fat, the present invention realizes saponification and microcapsule formation using simple method. Comparing to conventional absorption processes, the present invention effectively improves the chemical stability of lutein in light, heating and acid environment, allowing the controlled release type lutein feed additive product to barely release in gastric fluid environment but fully release in intestinal fluid environment, hence achieving higher bioavailability.

Compound, extract isolated from antrodia camphorate, and method of inhibiting cancer cell growth

Disclosed is a compound isolated from Antrodia camphorata , represented by formula I: wherein R1 is a hydrogen atom or an acetyl group; and a method of inhibiting cancer cell growth by using the compound, the cancer is selected from the group consisting of lung cancer, colon cancer, prostate cancer, liver cancer and breast cancer.

PROCESS FOR PREPARING CYCLIC ALPHA-KETO ALCOHOLS FROM CYCLIC ALPHA-KETO ENOLS

The invention relates to a method for preparing a cyclic α-ketoalcohol, particularly a 6-hydroxycyclohexenone from a cyclic α-ketoenol, particularly a 6-hydroxycyclohexadienone, using a reducing agent. This reducing agent is selected from hydrogen gas; a secondary alcohol, formic acid and the salts of formic acid or a mixture of at least two representatives of these compound classes. The invention further comprises the use of an α-ketoenol, in particular a 6-hydroxycyclohexadienone, as intermediate for preparing astaxanthin. 115.-. (canceled)17. The method according to claim 16 , wherein the reducing agent is at least one compound selected from the group consisting of hydrogen gas; a secondary alcohol; formic acid and the salts of formic acid.18. The method according to claim 16 , wherein the reducing agent is at least one compound selected from the group consisting of hydrogen gas; isopropanol or butan-2-ol; formic acid claim 16 , an alkali metal claim 16 , alkaline earth metal or ammonium formate or a mono- claim 16 , di- claim 16 , tri- or tetra(C1-C4)-alkylammonium formate.19. The method according to claim 16 , wherein the 6-hydroxycyclohexadienone is reacted non-stereoselectively or stereoselectively with the reducing agent in the presence of a transition metal catalyst.20. The method according to claim 16 , wherein the 6-hydroxycyclohexadienone is reacted non-stereoselectively or stereoselectively with the reducing agent in the presence of an achiral or optically active transition metal catalyst.21. The method according to claim 18 , wherein the transition metal catalyst comprises a transition metal selected from the group consisting of Ti claim 18 , Zr claim 18 , Hf claim 18 , V claim 18 , Nb claim 18 , Ta claim 18 , Cr claim 18 , Mo claim 18 , W claim 18 , Mn claim 18 , Re claim 18 , Fe claim 18 , Ru claim 18 , Os claim 18 , Co claim 18 , Rh claim 18 , Ir claim 18 , Ni claim 18 , Pd claim 18 , Pt claim 18 , Cu claim 18 , Ag and Au.22. The method according to ...

PROCESS FOR THE PRODUCTION OF 1,3,3-TRIMETHYL-2-(3-METHYLPENT-2-EN-4-YNYL)CYCLOHEX-1-ENE

The present invention relates to an improved process for the production of 1,3,3-trimethyl-2-(3-methylpent-2-en-4-ynyl)cyclohex-1-ene, highly enriched in the Z-isomer, and the use of such compounds in organic syntheses, especially in processes forming intermediates (building blocks) the synthesis of vitamin A or β-carotene or other carotenoids, e.g. canthaxanthin, astaxanthin or zeaxanthin. 2. Process according to claim 1 , wherein the process is carried out at a temperature of between 40° C. and 100° C. claim 1 , preferably between 50° C. and 80° C.3. Process according to claim 1 , wherein the process is carried out at ambient pressure.4. Process according to claim 1 , wherein the process is carried out using thiolate-bridged diruthenium complexes and optionally a weakly coordinating anion as catalyst system.5. Process according to claim 1 , wherein the process is carried out using [(C(CH))RuCl(.-SMe)Ru(C(CH))Cl] and ammonium tetrafluoroborate as a catalyst system.6. Process according to claim 1 , wherein the process is carried out in a water-free solvent (or mixture of solvents).8. Use of a compound of formula (Ia) in organic synthesis.9. Use according to claim 8 , wherein compound of formula (Ia) is used to produce intermediates useful in the synthesis of vitamin A claim 8 , -carotene claim 8 , canthaxanthin claim 8 , astaxanthin claim 8 , zeaxanthin. The present invention relates to an improved process for the production of 1,3,3-trimethyl-2-(3-methylpent-2-en-4-ynyl)cyclohex-1-ene, as well as to an isomerically highly enriched form thereof and the use of such compounds in organic syntheses, especially in processes forming intermediates (building blocks) for the synthesis of vitamin A or β-carotene or other carotenoids, e.g. canthaxanthin, zeaxanthin or astaxanthin. Especially to be mentioned is that the new compounds are useful as starting materials for the synthesis of vitamin A.is an important ingredient for many applications. Vitamin A plays a role in a ...

METHOD FOR PRODUCING ASTAXANTHIN FROM ASTACIN

The invention relates to a method for the non-stereoselective and also for the stereoselective synthesis of astaxanthin from astacin. For this purpose, a reducing agent is used selected from the group of hydrogen, a secondary alcohol, formic acid and also the salts of formic acid or from a mixture of at least two representatives of the compound classes stated above. The invention further relates to the use of astacin as starting compound for the synthesis of astaxanthin. 115-. (canceled)17. The method according to claim 16 , wherein the reducing agent is at least one compound selected from the group consisting of hydrogen gas; a secondary alcohol claim 16 , formic acid or the salts of formic acid.18. The method according to claim 16 , wherein the reducing agent is at least one compound selected from the group consisting of hydrogen gas; isopropanol; butan-2-ol; formic acid claim 16 , an alkali metal claim 16 , alkaline earth metal or ammonium formate or a mono- claim 16 , di- claim 16 , tri- or tetra(C1-C4)-alkylammonium formate.19. The method according to claim 16 , where in the astacin (2) is reacted non-stereoselectively or stereoselectively with the reducing agent in the presence of a transition metal catalyst.20. The method according to claim 16 , wherein the astacin (2) is reacted non-stereoselectively or stereoselectively with the reducing agent in the presence of an achiral or optically active transition metal catalyst.21. The method according to claim 18 , wherein the transition metal catalyst comprises a transition metal selected from the group consisting of Ti claim 18 , Zr claim 18 , Hf claim 18 , V claim 18 , Nb claim 18 , Ta claim 18 , Cr claim 18 , Mo claim 18 , W claim 18 , Mn claim 18 , Re claim 18 , Fe claim 18 , Ru claim 18 , Os claim 18 , Co claim 18 , Rh claim 18 , Ir claim 18 , Ni claim 18 , Pd claim 18 , Pt claim 18 , Cu claim 18 , Ag and Au.22. The method according to claim 18 , wherein the transition metal catalyst comprises a transition ...

CATALYTIC ETHYNYLATION

The present invention relates to the catalytic ethynlation of αβ-unsaturated ketones for producing tertiary acetylenic alcohols. 2. Process according to claim 1 , whereinR is an aliphatic or aromatic hydrocarbon which is substituted with lower alkoxy or lower alkyl groups and{'sub': 1', '3, 'Ris CH.'}4. Process according to claim 1 , wherein the process is carried out at a temperature below +5° C.5. Process according to claim 1 , wherein the process is carried out at a temperature of from −60° C. to 5° C.6. Process according to claim 1 , wherein the process is carried out at atmospheric conditions.7. Process according to claim 1 , wherein the process is carried out at elevated pressure.8. Process according to claim 1 , herein the process is carried without any addition of water. The present invention relates to the catalytic ethynylation of α,β-unsaturated ketones for producing tertiary acetylenic alcohols.The ethynyated reaction products, α-alkynols, are important intermediates in organic synthesis. For example, ethynyl-β-ionol is an intermediate used in the preparation of vitamin A and β-carotene.The process for ethynylating of α,β-unsaturated ketones for producing tertiary acetylenic alcohols is well known and described in many patent (i.e. in U.S. Pat. Nos. 3,709,946; 3,082,260, 3,283,014, 4,147,886 and 4,320,236).In U.S. Pat. No. 4,320,236, the ethynylation is carried out in the presence of a monolithium acetylide-ammonia complex.In U.S. Pat. No. 4,147,886, the ethynylation is carried out in the presence of diluted KOH.Due to the importance of the ethynylated reaction products, there is always a need for an improved way to producing such products.Surprisingly, it was found that the use of solid KOH in the reaction process allows to carry out the ethynylation process in an easy way.Therefore, the present invention relates to a process (P) to produce compounds of formula (III)whereinR is hydrogen or an aliphatic, cyclo-aliphatic or aromatic hydrocarbon which can ...

PROCESS FOR THE PRODUCTION OF 1,3,3-TRIMETHYL-2-(3-METHYLPENT-2-EN-4-YNYL)CYCLOHEX-1-ENE

The present invention relates to an improved process for the production of 1,3,3-tri-methyl-2-(3-methylpent-2-en-4-ynyl)cyclohex-1-ene, highly enriched in the Z-isomer, and the use of such compounds in organic syntheses, especially in processes forming intermediates (building blocks) the synthesis of vitamin A or β-carotene or other carotenoids, e.g. canthaxanthin, astaxanthin or zeaxanthin. 2. A product comprising more than 85% of (Z)-1 ,3 ,3-trimethyl-2-(3-methylpent-2-en-4-ynyl)cyclohex-1-ene.3. An process for synthesizing organic molecules which comprises providing the compound of formula (Ia) according to as an intermediate compound claim 1 , and synthesizing an organic molecule from the intermediate compound of fomula (Ia) by subjecting the intermediate compound of formula (Ia) to organic molecule synthesis reaction conditions.4. The process of claim 3 , wherein organic molecule synthesized from the intermediate compound of formula (Ia) is selected from the group consisting of vitamin A claim 3 , β-carotene claim 3 , canthaxanthin claim 3 , astaxanthin and zeaxanthin. This application is a continuation of commonly owned copending U.S. application Ser. No. 14/128,741, filed May 28, 2014 (now U.S. Pat. No. ______), which is the national phase application under 35 USC §371 of PCT/EP2012/061280, filed Jun. 14, 2012 which designated the U.S. and claims the benefit of priority of EP 11171068.7, filed Jun. 22, 2011, the entire contents of which are hereby incorporated by reference.The present invention relates to an improved process for the production of 1,3,3-trimethyl-2-(3-methylpent-2-en-4-ynyl)cyclohex-1-ene, as well as to an isomerically highly enriched form thereof and the use of such compounds in organic syntheses, especially in processes forming intermediates (building blocks) for the synthesis of vitamin A or β-carotene or other carotenoids, e.g. canthaxanthin, zeaxanthin or astaxanthin. Especially to be mentioned is that the new compounds are useful as ...

Cyclohexenone Compositions and Process for Making Thereof

Provided herein are processes of preparing cyclohexenone compounds useful for cancer treatments and/or diseases. 2. The process of claim 1 , X is an oxygen claim 1 , Y is an oxygen.4. The process of claim 3 , X is an oxygen claim 3 , Y is an oxygen.5. The process of claim 1 , wherein each of R claim 1 , Rand Rindependently is H claim 1 , methyl claim 1 , ethyl claim 1 , propyl claim 1 , butyl claim 1 , pentyl or hexyl.6. The process of claim 1 , wherein said base is a lithium salt.7. The process of claim 6 , wherein said lithium salt is n-butyllithium.8. The process of claim 3 , wherein said enolate compound is prepared under basic conditions.9. The process of claim 3 , wherein said enol compound is prepared under acidic conditions.10. The process of claim 3 , wherein Ris an acyclic or cyclic acetal claim 3 , acyclic or cylic ketal claim 3 , dithio acetal claim 3 , dithio ketal claim 3 , cyclic dithio acetal claim 3 , cyclic dithio ketal claim 3 , substituted hydrazone claim 3 , oxime claim 3 , oxime derivative claim 3 , or oxazolidine.13. The process of claim 12 , wherein X is an oxygen claim 12 , Y is an oxygen.14. The process of claim 12 , wherein Ris methyl substituted with phenyl.15. The process of claim 12 , wherein Ris methyl substituted with phenyl.16. The process of claim 12 , wherein said base is a lithium salt.17. The process of claim 16 , wherein said lithium salt is n-butyllithium. The present disclosure relates to composition and processes of preparing cyclohexenone compounds.In one aspect, there are provided a process for preparing a compound of formula I:comprising a step of reacting a compound of formula II,with a compound of formula (III), PhPCHRRL (III) in the presence of a base, wherein L is a leaving group, P1 is a hydroxyl protecting group; each of X and Y independently is a bond, oxygen, NRor sulfur;In another aspect, there are provided processes for preparing a compound of formula Ia:comprising a step of reacting a compound of formula IIa, ...

ETHYNYLATION OF POLYUNSATURATED ALDEHYDES AND KETONES

The present invention relates to a catalytic process for the ethynylation of specific polyunsaturated aldehydes and ketones. 5. The catalytic ethynylation process according to claim 1 , wherein the catalyst is added to the reaction mixture as an aqueous solution.6. The catalytic ethynylation process according to claim 1 , wherein R is K.7. The catalytic ethynylation process according to claim 1 , wherein the catalytic ethynylation reaction is carried out under pressure which is in a range from 2 bar to 15 bar.8. The catalytic ethynylation process according to claim 1 , wherein the catalytic ethynylation reaction temperature is between −30° to 5° C.9. The catalytic ethinylation process according to claim 1 , wherein the catalytic ethynylation reaction is carried out under pressure which is in a range of 5 bar to 12 bar.10. The catalytic ethinylation process according to claim 1 , wherein the catalytic ethynylation reaction is carried out under pressure which is in a range of 6 bar to 10 bar. This application is a continuation of commonly owned copending U.S. application Ser. No. 15/518,080, filed Apr. 10, 2017 (now abandoned), which is the U.S. national phase of International Application No. PCT/EP2015/073868 filed Oct. 15, 2015, which designated the U.S. and claims priority to EP Patent Application No. 14189262.0, filed Oct. 16, 2014, the entire contents of each of which are hereby incorporated by reference.The present invention relates to a catalytic process for the ethynylation of specific polyunsaturated aldehydes and ketones.Polyunsaturated aldehydes and ketones in the context of the present invention are aldehydes and ketones wherein the aldehydes and ketones comprise at least two C—C double bonds. In some embodiments of the present invention the C—C double bonds can also be conjugated.Polyunsaturated aldehydes and ketones (with conjugated C—C double bonds), such as the α,β-unsaturated ones, are quite stable compounds.The reaction products, which are the ...

PROCESS FOR PREPARING ALPHA-DAMASCONE

The present invention relates to a process for preparing 1-(2,6,6-trimethylcyclohex-2-en-1-yl)but-2-en-1-one, which comprises a) providing 6,10-dimethylundeca-1,5,9-trien-4-ol, b) oxidizing 6,10-dimethylundeca-1,5,9-trien-4-ol provided in step a) with an oxidizing agent in the presence of at least one organic nitroxyl radical, at least one nitrate compound and an inorganic solid to yield 6,10-dimethylundeca-1,5,9-trien-4-one, c) reacting the 6,10-dimethylundeca-1,5,9-trien-4-one obtained in step b) with an acid to yield 1-(2,6,6-trimethylcyclohex-2-en-1-yl)but-2-en-1-one. 115.-. (canceled)16. A process for preparing 1-(2 ,6 ,6-trimethylcyclohex-2-en-1-yl)but-2-en-1-one , comprising:a) providing 6,10-dimethylundeca-1,5,9-trien-4-ol,b) oxidizing the 6,10-dimethylundeca-1,5,9-trien-4-ol provided in step a) with an oxidizing agent, which is selected from the group consisting of hypochlorites, hydrogen peroxide and molecular oxygen, in the presence of at least one organic nitroxyl radical, at least one nitrate compound and an inorganic solid, which is selected from the group consisting of alkali metal halides and alkali earth metal halides, to yield 6,10-dimethylundeca-1,5,9-trien-4-one,c) reacting the 6,10-dimethylundeca-1,5,9-trien-4-one obtained in step b) with an acid selected from mineral acids to yield 1-(2,6,6-trimethylcyclohex-2-en-1-yl)but-2-en-1-one.17. The process of claim 16 , where the total amount of the at least one nitroxyl radical used in step b) is in the range of 1 to 50 mol-% claim 16 , based on the amount of 6 claim 16 ,10-dimethylundeca-1 claim 16 ,5 claim 16 ,9-trien-4-ol in the reaction mixture.18. The process according to claim 16 , where the nitroxyl radical used in step b) is selected from the group consisting of (2 claim 16 ,2 claim 16 ,6 claim 16 ,6-tetramethylpiperidin-1-yl)oxyl compounds claim 16 , 2-azaadamantane-N-oxyl compounds claim 16 , (1 claim 16 ,1 claim 16 ,3 claim 16 ,3-tetramethylisoindolin-2-yl)oxyl compounds claim 16 , 9- ...

Processes for the preparation of hydroxylated cyclohexyl compounds

The present application relates to processes for the preparation of polyhydroxylated cyclohexyl compounds such as the compounds of Formula I:

4-OXO-N-(4-HYDROXYPHENYL)RETINAMIDE DERIVATIVES AS THERAPEUTIC AGENTS FOR THE TREATMENT OF CANCER

The present invention relates to a compound having formula (I) below or a pharmaceutically acceptable salt thereof: 2. The compound of formula (I) or a pharmaceutically acceptable salt thereof according to wherein X is —COOH.3. The salt of a compound of formula (I) according to with an alkali or alkaline-earth metal claim 2 , an organic amine or an amino acid.4. The salt of a compound of formula (I) according to with sodium claim 3 , potassium claim 3 , lithium claim 3 , calcium or magnesium.5. The compound of formula (I) or a pharmaceutically acceptable salt thereof according to claim wherein X is NH.6. The compound of formula (I) or a pharmaceutically acceptable salt thereof according to wherein R is a straight or branched C-Calkylene chain.7. The compound of formula (I) or a pharmaceutically acceptable salt thereof according to wherein Ris H.8. A compound of formula (I) according to selected from the group consisting of:sodium 2-[3-[(1E,3E,5E,7E)-9-(4-hydroxyanilino) -3,7-dimethyl-9-oxo-nona-1,3,5,7-tetraenyl]-2,4,4-trimethyl-cyclohex-2-en-1-ylidene]amino]oxyacetate (compound 1a);sodium 2-[3-[(1E,3E,5E,7E)-9-(4-hydroxyanilino)-3,7-dimethyl-9-oxo-nona-1,3,5,7-tetraenyl]-2,4,4-trimethyl-cyclohex-2-en-1-ylidene]amino]oxybutyrate (compound 1b);sodium 2-[3-[(1E,3E,5E,7E)-9-(4-hydroxyanilino)-3,7-dimethyl-9-oxo-nona-1,3,5,7-tetraenyl]-2,4,4-trimethyl-cyclohex-2-en-1-ylidene]amino]oxyhexanoate (compound 1c).9. A medicament comprising the compound of formula (I) or a pharmaceutically acceptable salt thereof according to .10. An antitumoral or chemopreventive agent comprising the compound of formula (I) or a pharmaceutically acceptable salt thereof according to .11. A method for treatment of solid or haematological claim 10 , both metastatic and non-metastatic claim 10 , tumors claim 10 , comprising providing and applying an effective amount of the antitumoral or chemopreventive agent according to .12. The method according to claim 11 , wherein the treatment is that of ...

INHIBITORS OF RETINALDEHYDE DEHYDROGENASES AND METHODS OF USE

Compounds having inhibitory activity against retinaldehyde dehydrogenases (RALDHs). The compounds can be used, for example, to inhibit synthesis of retinoic acid for the treatment of refractive error disorders such as myopia, and as infertility treatments by inhibiting spermatogenesis. 2. The compound of claim 1 , wherein X is C.3. The compound of claim 1 , wherein X is O.4. The compound of claim 1 , wherein X is NH.5. The compound of claim 1 , wherein at least one of Rand Ris Cl.6. The compound of claim 1 , wherein at least one of R claim 1 , R claim 1 , and Ris CH.7. The compound of claim 1 , wherein at least one of R claim 1 , and Ris CH.8. The compound of claim 1 , wherein at least one of Rand Ris Cl claim 1 , and at least one of R claim 1 , R claim 1 , and Ris CH.9. The compound of claim 1 , wherein at least one of Rand Ris Cl claim 1 , and at least one of R claim 1 , and Ris CH.10. The compound of claim 1 , wherein at least one of R claim 1 , R claim 1 , and Ris CH claim 1 , and at least one of R claim 1 , and Ris CH.11. The compound of claim 1 , wherein at least one of Rand Ris Cl claim 1 , at least one of R claim 1 , R claim 1 , and Ris CH claim 1 , and at least one of R claim 1 , and Ris CH.12. The compound of claim 1 , wherein Rand Rare Cl claim 1 , and Rand Rare CH.13. The compound of claim 1 , wherein Rand Rare Cl claim 1 , and Rand Rare CH.14. The compound of claim 1 , wherein Rand Rare CH claim 1 , and R claim 1 , and Rare CH.15. The compound of claim 1 , wherein Rand Rare Cl claim 1 , and Rand Rare CH claim 1 , and Rand Rare CH.16. The compound of claim 1 , wherein Rand Rare Cl claim 1 , and R claim 1 , R claim 1 , R claim 1 , R claim 1 , and Rare CH.17. A composition claim 1 , comprising the compound of disposed in a pharmaceutically-acceptable carrier claim 1 , vehicle claim 1 , or diluent.18. A method of controlling claim 1 , reducing claim 1 , or inhibiting synthesis of retinoic acid in a subject in need of a therapy responsive to such inhibitory ...

RETINOID DOUBLE CONJUGATE COMPOUNDS, COMPOSITIONS THEREOF, AND METHODS FOR TREATING OF SKIN CONDITIONS

A double conjugate molecule made of a retinoid, an organic acid, particularly an α-hydroxy acid, and an alcohol or acyl group, is provided which is useful in treating skin conditions, particularly aging. The retinoid, organic acid, and alcohol/acyl group are preferably linked via ester bonds. 2: The molecule of claim 1 , wherein{'sub': 2', 'a', '2', 'a, 'X is independently (CO)O, O(OC), O—(CH), (CH)—O, (CO)N, or N(CO),'}a is 0 or 1,k is 1 or 2,m is 0, 1, 2, 3, 4, 5, 6, or 7,n is 0, 1, 2, or 3,{'sub': 1', '2', '3', '4', '5', '1', '2', '4', '5, 'R, R, R, R, R, and Rare independently H, COOH, CHO, alkyl comprising 1 to 15 carbon atoms optionally substituted by one or more OH or interrupted by one or more O, (alk)aryl comprising 1 to 15 carbon atoms, optionally substituted by one or more OH or interrupted by one or more O, or one or more pairs of Rand Ror R, and Rforms a carbonyl,'}{'sub': 6', '7', '8', '9', '9', '9', '9', '9', '9', '9', '9', '9', '9, 'R, R, and Rare independently H, alkyl comprising 1 to 15 carbon atoms optionally substituted by OH, CHO, COOR, CROR, or CONRR, or (alk)aryl comprising 1 to 15 carbon atoms optionally substituted by OH, CHO, COOR, CROR, or CONRR, and'}{'sub': '9', 'Ris independently H or alkyl comprising 1 to 5 carbon atoms.'}3: The molecule of claim 1 , wherein{'sub': 2', 'a', '2', 'a, 'X is independently (CO)O, O(OC), O—(OH), or (CH)—O,'}a is 0 or 1,k is 1,m is 0, 1, 2, or 3,n is 0 or 1{'sub': 1', '2', '3', '4', '5', '1', '2', '4', '5, 'R, R, R, R, R, and Rare independently H, COOH, CHO, alkyl comprising 1 to 10 carbon atoms optionally substituted by one or more OH or interrupted by one or more O, (alk)aryl comprising 1 to 7 carbon atoms, optionally substituted by one or more OH or interrupted by one or more O, or one or more pairs of Rand Ror R, and Rforms a carbonyl,'}{'sub': 6', '7', '8', '9', '9', '9', '9', '9', '9', '9', '9', '9', '9, 'R, R, and Rare independently H, alkyl of 1 to 10 carbon atoms optionally substituted by OH, CHO, ...

ABSCISIC ACID DERIVATIVE

The compound represented by formula (IV) or a salt thereof has an inhibitory action on an abscisic acid receptor. The compound or the salt thereof can be used as a plant growth regulator. 3. The compound or the salt thereof according to claim 2 , wherein Ris a phenyl group or a 1-naphthyl group.4. An inhibitor of an abscisic acid receptor claim 1 , comprising the compound or the salt thereof according to .5. A plant growth regulator comprising the compound or the salt thereof according to .6. An inhibitor of an abscisic acid receptor claim 2 , comprising the compound or the salt thereof according to .7. An inhibitor of an abscisic acid receptor claim 3 , comprising the compound or the salt thereof according to .8. A plant growth regulator comprising the compound or the salt thereof according to .9. A plant growth regulator comprising the compound or the salt thereof according to . The present invention relates to an abscisic acid derivative. More specifically, the present invention relates to an abscisic acid receptor antagonist.Abscisic acid is a phytohormone playing an important role in the seed dormancy and the environmental stress response. The abscisic acid receptor, when bonded to abscisic acid, changes the three-dimensional conformation thereof and bonds to protein phosphatase PP2C to inhibit the enzyme activity thereof, thereby activating the signal transduction thereafter.Abscisic acid receptor antagonists are expected to be applied to the agricultural field as the plant growth regulator and, in recent years, it has been reported that an abscisic acid derivative obtained by introducing an alkyl sulfanyl group into the 3′-position of abscisic acid has the abscisic acid receptor antagonistic action (Non Patent Literature 1).Non Patent Literature 1: Takeuchi et al., “Designed abscisic acid analogs as antagonists of PYL-PP 2C receptor interactions”, Nature Chemical Biology, vol.10, pp.477-482 (2014)The present invention has an object to provide a novel abscisic ...

METHOD FOR PRODUCING N-RETINOYLCYSTEIC ACID ALKYL ESTER

A method for producing derivatives of N-retinoylaminoalkane sulfonic acid, the method comprising providing retinoic acid, chloroformate, aminoalkanesulfonic acid selected from the group consisting of cysteic acid and alkyl ester thereof, cysteinesulfinic acid and alkyl ester thereof, homocysteic acid and alkyl ester thereof, homocysteinesulfinic acid and alkyl esters thereof, taurine and derivatives thereof, and an organic solvent, and a base, mixing said components under substantial absence of oxidizing compounds thereby forming a reaction mixture comprising a liquid phase, wherein the liquid phase is one phase and the derivatives of N-retinoylaminoalkane sulfonic acid are formed in said liquid phase. 1. A method for producing derivatives of N-retinoylaminoalkane sulfonic acid , the method comprising providingi) a first solution comprising an aminoalkane sulfonic acid selected from the group consisting of cysteic acid and alkyl ester thereof, cysteinesulfinic acid and alkyl ester thereof, homocysteic acid and alkyl ester thereof, homocysteinesulfinic acid and alkyl esters thereof, taurine and derivatives thereof, an alcohol selected from aliphatic alcohols comprising 1 to 4 carbon atoms and a first base selected from trialkylamines,ii) a second solution comprising a retinoic acid, a chloroformate, an aprotic solvent and a second base,adding first and second solutions in any order to a reaction vessel thereby forming a reaction mixture comprising at least a liquid phase being one phase, mixing said reaction mixture, wherein retinoic acid, aminoalkane sulfonic acid and chloroformate are all soluble and present in said liquid phase and the derivatives of N-retinoylaminoalkane sulfonic acid are formed in said liquid phase under conditions characterised as being substantially free from oxidizing compounds.2. The method according to claim 1 , wherein the derivatives of N-retinoylaminoalkane sulfonic acid are selected from N-(13-cis-retinoyl)-cysteic acid alkyl ester and ...

Novel Plant Growth Regulators and Methods of Using Same

This disclosure relates to methods of regulating growth in a plant. Specifically, the methods of the disclosure regulate growth of the plant by administration of a composition comprising an effective amount of one or more apocarotenoids to the plant, its part, or the seed. 1. A method for regulating growth in a plant , the method comprising exogenously contacting a composition comprising an effective amount of one or more apocarotenoids to the plant , a plant part , or a plant seed.2. The methods of claim 1 , wherein regulating comprises improving growth of a plant.3. The method of claim 2 , wherein the improving growth comprises modifying the root architecture of the plant.4. The method of claim 2 , wherein the improving growth alters lateral root formation in the plant.5. The method of claim 2 , wherein the growth of the plant is improved by at least about 10% compared to the plant not contacted with the composition.6. The method of claim 2 , wherein regulating comprises reducing the growth of a plant.7. A method for improving drought tolerance in a plant claim 2 , the method comprising exogenously contacting a composition comprising an effective amount of one or more apocarotenoids to the plant claim 2 , a plant part claim 2 , or a plant seed.8. The method of claim 1 , wherein contacting is by irrigating the plant.9. A method for fertilizing plant soil claim 1 , the method comprising providing a composition comprising an effective amount of one or more apocarotenoids to the soil.10. The method according to claim 9 , wherein fertilizing is by irrigation.11. The method according to claim 1 , wherein the apocarotenoid is selected from the group consisting of β-ionone claim 1 , β-cyclocitral claim 1 , safranal claim 1 , dihydro-β-Ionone claim 1 , dimethyl-β-cyclocitral claim 1 , dihydroactinidiolide (DHAD) claim 1 , α-ionone claim 1 , pseudoionone claim 1 , retinal claim 1 , 2 claim 1 ,6 claim 1 ,6-trimethyl-1-cyclohexene-1-carboxylic acid claim 1 , 2 claim 1 ,6 ...

Improved process for preparing astacene

The invention describes a process for making astacene of formula 1, the exocyclic double bonds thereof having either an E configuration or an E- and/or Z-configuration, wherein astaxanthin of the general formula 2 having asymmetric centers 3 and 3′, each of which respectively having an (S)- or (R)-conformation and the exocyclic double bonds of said astaxanthin 2 having either an E- or E- and/or Z configuration, is oxidized in the presence of at least one tertiary alcoholate.

METHOD FOR PRODUCING ASTAXANTHIN ESTERS

The invention describes an environmentally friendly, sustainable and cost-effective method for preparing astaxanthin diesters of the formula 1, in which astaxanthin of the formula 2 is doubly esterified with fatty acid chlorides of the general formula 3. For this purpose, compound 2 and 3 are reacted in an organic solvent in the presence of a nitrogen-containing base of the general formula 4. The invention further relates to the non-therapeutic use of the diester 1, in which R is a residue selected from the group consisting of C13-C19-alkyl, C13-C19-alkenyl, C13-C19-alkdienyl and C13-C19-alktrienyl, in human or animal nutrition and also the therapeutic use of the diester 1 prepared according to the method as a medicament and also as an ingredient in a medicinal preparation. 2. The method according to claim 1 , wherein the astaxanthin of the formula (2) in the organic solvent is reacted with a greater than two-fold molar excess claim 1 , based on astaxanthin (2) claim 1 , of the acid chloride of the formula (3) in the presence of at least one nitrogen-containing base of the formula (4).3. The method according to claim 1 , wherein the astaxanthin of the formula (2) in the organic solvent is reacted with a 2.3-fold to 7-fold molar excess claim 1 , of the acid chloride of the formula (3) in the presence of at least one nitrogen-containing base of the formula (4).4. The method according to claim 1 , wherein the organic solvent is a chlorine-containing organic solvent selected from the group consisting of dichloromethane claim 1 , trichloromethane claim 1 , tetrachloromethane claim 1 , 1 claim 1 ,1-dichloroethane claim 1 , 1 claim 1 ,2-dichloroethane claim 1 , trichloroethylene claim 1 , tetrachloroethylene claim 1 , perchloroethylene claim 1 , chlorobenzene or a mixture of at least two of the chlorine-containing organic solvents.5. The method according to claim 4 , wherein the astaxanthin of the formula (2) in the organic solvent is reacted with the acid chloride of the ...

PROCESS FOR PURIFYING ASTAXANTHIN AND CANTHAXANTHIN

The present invention relates to a process for purifying the xanthophylls astaxanthin and canthaxanthin. 119.-. (canceled)21. The process according to claim 20 , wherein the ketone of the formula (I) makes up at least 99% by weight of the organic solvents used for the suspension.22. The process according to claim 20 , wherein the concentration of water in the solvent used to produce the suspension does not exceed 20% by weight.23. The process according to claim 20 , wherein the suspension is treated at a temperature in the range from 60 to 150° C.24. The process according to claim 20 , wherein the treatment time of treating the suspension is in the range from 6 to 144 h.25. The process according to claim 20 , wherein the suspension has a xanthophyll concentration in the range from 2 to 50% by weight.26. The process according to claim 20 , wherein claim 20 , in the course of the treatment claim 20 , at least some of the ketone of the formula (I) is distilled off and replaced by fresh ketone of the formula (I).27. The process according to claim 20 , wherein the suspension is cooled to a temperature below 20° C. before separating off the xanthophyll from the organic solvent.28. The process according to claim 20 , wherein the ketone is selected from compounds of the general formula (I) and mixtures thereof claim 20 , where Ris methyl or ethyl and Ris C-Calkyl.29. The process according to claim 20 , wherein a suspension of the xanthophyll in a ketone of the formula (I) claim 20 , where Ris methyl or ethyl and Ris C-Calkyl claim 20 , is first treated at elevated temperature and the xanthophyll thus obtained is treated with acetone.30. The process according to claim 20 , wherein the treatment of the suspension of the xanthophyll in the organic solvent and the subsequent separation off of the xanthophyll from the solvent is repeated at least once.31. The process according to claim 20 , wherein the xanthophyll used contains one or more halogenated hydrocarbons as contaminant ...

2-(ALKOXY OR ARYLOXY CARBONYL)-4-METHYL-6-(2,6,6-TRIMETHYLCYCLOHEX-1- ENYL)HEX-2-ENOIC ACID COMPOUNDS, ITS PREPARATION AND USE

Compounds of the formula 1 2. The compound according to wherein R is methyl.3. The compound according to wherein R is ethyl.7. The method according to wherein the organocatalyst is selected from the group consisting of ammonium salts of carboxylic acids claim 6 , ammonium salts of polycarboxylic acids claim 6 , and amine components selected from the group consisting of ammonia claim 6 , primary amines claim 6 , secondary amines claim 6 , polyamines claim 6 , amino acids and peptides.8. The method according to wherein the solvent or solvent system forms an azeotrope with water claim 6 , which is constantly removed from the reaction mixture by distillation.9. The method according to wherein the condensation reaction is carried out at about 60-95° C.10. The method according to wherein the solvents are selected from cyclohexane claim 6 , benzene claim 6 , toluene claim 6 , iso-propanol and tert-butanol. The present application is a continuation of co-pending U.S. Ser. No. 14/854,705, filed Sep. 15, 2015, which is a divisional application of U.S. Ser. No. 14/563,312, filed Dec. 8, 2014, now U.S. Pat. No. 9,163,000, which is a divisional application of U.S. Ser. No. 13/995,368, having a 35 USC 371 (c) date of Nov. 27, 2013, now U.S. Pat. No. 8,933,253, which is a national stage application of International Application No. PCT/EP2011/73550, filed Dec. 21, 2011, which claims the benefit of Great Britain Application No. 1021584.6, filed Dec. 21, 2010, which applications are incorporated herein by reference.The invention is concerned with organic compounds their preparation and use as intermediates in the synthesis of fragrance ingredients.Many fragrance ingredients that are used by perfumers in the creation of new and exciting fragrance accords are commodity ingredients, that is, they are non-proprietary and versions of the ingredients, which may differ in price and quality, and are available from many different suppliers. The uptake of a particular version of such ...

PROCESS OF PRODUCTION OF 7,8-DIHYDRO-C15-ALDEHYDE

The present invention relates to a new method to produce 7,8-dihydro-C-aldehyde. 2. Process according to claim 1 , wherein step (1) is carried out by a Grignard reaction.3. Process according to claim 1 , wherein step (1) is carried out by a catalytic reaction step.5. Process according to claim 3 , wherein the pressure in step (2) is in the range from 2 bar to 15 bar.6. Process according to claim 3 , wherein the reaction temperature step (2) is between −40° C.-10° C.7. Process according to anyone claim 1 , wherein the rearrangement (step (2)) is carried out by using at least one transition metal-based catalyst.8. Process according to claim 7 , wherein the rearrangement is carried out by using at least one Vanadium-based catalyst.9. Process according to claim 1 , wherein in step (2) the substrate to catalyst ratio is from 5000:1 to 10:1 claim 1 , preferably from 1000:1 to 20:1.10. Process according to claim 1 , wherein the rearrangement (step (2) is carried out in at least one non polar or polar aprotic organic solvent in the presence of at least one organic acid having a pK value in the range of about 4.0 to about 6.5.11. Process according to claim 10 , wherein the non polar or polar aprotic organic solvent is chosen from the group consisting of aliphatic claim 10 , cyclic and aromatic hydrocarbons (such as C-C-alkanes claim 10 , C-C-cycloalkanes claim 10 , benzene claim 10 , toluene naphthalene claim 10 , paraffin oil) and carboxylate esters (such as ethyl acetate).12. Process according to claim 10 , wherein the organic acid is chosen from the group consisting of acetic acid claim 10 , propionic acid claim 10 , chloropropionic acid claim 10 , pivalic acid claim 10 , acrylic acid claim 10 , adipic acid claim 10 , phenylacetic acid claim 10 , benzoic acid and 4-tert.butyl-benzoic acid.13. Process according to claim 1 , wherein the rearrangement (step (2)) is carried out at a reaction temperature of 10° C. to 50° C. claim 1 , preferably 20° C. to 40° C. The present ...

Carotenoid Compound Coming From Plant And Containing Natural Astaxanthin, Preparation Method Therefor, And Composition

The present invention provides a high-content carotenoid compound from . The content of the total carotenoid of the carotenoid compound is greater than 95%. The content of all-trans (3S, 3′S)-carotenoid is greater than 80%. The carotenoid crystals have a high purity, and can be used in multiple forms in the fields of a dietary supplement of a human being, a food additive, a feed additive and a cosmetic product. In addition, the present invention also provides a method for manufacturing the compound. 2. The high-content carotenoid compound according to claim 1 , characterized in that claim 1 , the total carotenoid comprises semi-astacene claim 1 , astacene and adonirubin.3. The high-content of carotenoid compound according to claim 2 , characterized in that claim 2 , the proportion of the total content of semi-astancene and astacene in the total carotenoid is less than 10 wt % claim 2 , and the proportion of adonirubin in the total carotenoid is less than 10 wt %.4. A composition comprising the high-content carotenoid compound according to .5. The composition according to claim 4 , characterized in that claim 4 , further comprising one or more of vegetable oil claim 4 , modified starch claim 4 , sucrose claim 4 , dextrin and gelatin.6. A composition comprising the high-content carotenoid compound according to .7. The composition according to claim 6 , further comprising one or more of vegetable oil claim 6 , modified starch claim 6 , sucrose claim 6 , dextrin and gelatin.8. A composition comprising the high-content carotenoid compound according to .9. The composition according to claim 8 , further comprising one or more of vegetable oil claim 8 , modified starch claim 8 , sucrose claim 8 , dextrin and gelatin.11Adonis amurensisAdonis amurensis. The method according to claim 10 , characterized in that claim 10 , in step (a) claim 10 , the ratio of the volume of the alcohols solvent to the weight of extract is 5˜50 times claim 10 , preferably claim 10 , the ratio of ...

METHODS FOR SELECTIVE OXIDATION OF ALPHA TOCOTRIENOL IN THE PRESENCE OF NON-ALPHA TOCOTRIENOLS

A method of producing alpha-tocotrienol quinone or a stereoisomer thereof, the method comprising selective opening of alpha-tocotrienol chroman to alpha-tocotrienol quinone in the presence of non-alpha tocotrienol chromans by oxidizing alpha-to-cotrienol with a metal salt oxidizing agent, wherein the stoichiometric ratio of metal salt oxidizing agent/alpha-tocotrienol is at least 4:1 and wherein said metal oxidizing agent is added in sequential additions, in order to reduce oxidation of any amounts of non-alpha tocotrienol chromans that might have been present in the starting alpha-tocotrienol chroman material. This process uses conditions favoring oxidation rates of the alpha tocotrienol chroman vs. the non-alpha tocotrienol chromans. 115.-. (canceled)17. The method according to comprising oxidizing alpha-tocotrienol with the metal salt oxidizing agent in a biphasic solution claim 16 , wherein a first solution comprises the alpha-tocotrienol dissolved in a non-polar solvent; a second solution comprises the metal salt oxidizing agent dissolved in a polar solvent; and the separate first and second solutions are mixed to permit the oxidation.18. The method according to claim 16 , wherein the metal salt oxidizing agent is sufficient to oxidize at least about 98% of the alpha-tocotrienol into the alpha-tocotrienol quinone.19. The method according to claim 18 , wherein the composition resulting from the oxidation has less than about 1% of one or more compounds selected from the group consisting of alpha-tocotrienol claim 18 , beta-tocotrienol claim 18 , beta-tocotrienol quinone claim 18 , gamma-tocotrienol claim 18 , gamma-tocotrienol quinone claim 18 , delta-tocotrienol claim 18 , delta-tocotrienol quinone claim 18 , and combinations thereof.20. The method according to claim 18 , wherein the composition resulting from the oxidation has less than about 0.7% of one or more compounds selected from the group consisting of alpha-tocotrienol claim 18 , beta-tocotrienol claim ...

BETA-CRYPTOXANTHIN FROM PLANT SOURCE AND A PROCESS FOR ITS PREPARATION

The present invention provides beta-cryptoxanthin crystals from plant source and a process for its preparation. The present invention particularly relates to a process for the preparation of high purity beta-cryptoxanthin crystals comprising at least about 10% by weight total xanthophylls, of which at least about 75% by weight is trans-beta-cryptoxanthin and the remaining including beta-carotene, and trace amounts of trans-capsanthin and other carotenoids derived from the plant source, including capsicum fruits. The production of beta-cryptoxanthin crystals with high content of trans-beta-cryptoxanthin makes it ideal and suitable for use as a provitamin A source material and also has potential effects on improving bone health and inhibiting bone resorption. 143-. (canceled)44. A composition comprising beta-cryptoxanthin concentrate derived from plant material , wherein said concentrate comprises at least about 10% by weight total xanthophylls , of which at least about 75% by weight is trans-beta-cryptoxanthin.45. The composition of claim 44 , wherein the total xanthophylls comprise by-products selected from zeaxanthin claim 44 , trans-capsanthin claim 44 , beta-carotene claim 44 , trace amounts of other carotenoids such as capsorubin or violaxanthin claim 44 , and combinations thereof.46. The composition of claim 44 , wherein the composition further comprises a pharmaceutically acceptable ingredient or a food grade ingredient.47. A method for the treatment of rheumatoid claim 44 , inflammatory arthritis claim 44 , or bone diseases claim 44 , comprising administering to a patient in need thereof a therapeutically effective amount of a beta-cryptoxanthin concentrate derived from plant material claim 44 , wherein said concentrate comprises at least about 10% by weight total xanthophylls claim 44 , of which at least about 75% by weight is trans-beta-cryptoxanthin.48. A method for strengthening of bone claim 44 , comprising administering to a patient in need thereof a ...

BETA-CRYPTOXANTHIN FROM PLANT SOURCE AND A PROCESS FOR ITS PREPARATION

The present invention provides beta-cryptoxanthin crystals from plant source and a process for its preparation. The present invention particularly relates to a process for the preparation of high purity beta-cryptoxanthin crystals comprising at least about 10% by weight total xanthophylls, of which at least about 75% by weight is trans-beta-cryptoxanthin and the remaining including beta-carotene, and trace amounts of trans-capsanthin and other carotenoids derived from the plant source, including fruits. The production of beta-cryptoxanthin crystals with high content of trans-beta-cryptoxanthin makes it ideal and suitable for use as a provitamin A source material and also has potential effects on improving bone health and inhibiting bone resorption. 1. (canceled)2. A process for the preparation of a trans-beta-cryptoxanthin enriched concentrate from plant material comprising about 10-80% by weight total xanthophylls , of which about 75-98% by weight is trans-beta-cryptoxanthin , the process comprising:(a) mixing an oleoresin of plant material comprising xanthophylls esters with an aliphatic alcoholic solvent;(b) saponifying the xanthophylls esters present in the oleoresin with an alkali at an elevated temperature;(c) removing the aliphatic alcoholic solvent followed by addition of water to obtain a diluted resultant mixture;(d) adding a diluted organic acid to the diluted resultant mixture to form a water layer and a precipitated xanthophylls mass;(e) removing the water layer and washing the precipitated xanthophylls mass with a polar solvent;(f) drying the precipitated xanthophylls mass to obtain a crude xanthophylls mass;(g) washing the crude xanthophylls mass with a non-polar solvent and concentrating the non-polar solvent washings to obtain a concentrated crude xanthophylls mass;(h) transferring the concentrated crude xanthophylls mass to a silica gel column and washing with a non-polar solvent;(i) eluting the column with a mixture of non-polar and polar solvent ...

PROCESS FOR THE PREPARATION OF 1-(2,6,6-TRIMETHYLCYCLOHEXYL)-ALKAN-3-OLS

The present invention relates to a process for the preparation of 1-(2,6,6-trimethylcyclohexylyalkan-3-ols, in particular 1-(2,6,6-trimethylcyclohexyl)-hexan-3-ol. The invention further relates to 5-alkoxy-1-(2,6,6-trimethylcyclohexenyl)-1-alken-3-ones and the use of these as a fragrance or as flavor, to a fragrance containing composition and/or a fragranced product containing 5-alkoxy-1-(2,6,6-trimethylcyclohexenyl)-1-alken-3-ones and to a method for imparting or modifying a scent or a flavor to a composition by including said alkoxyalkenones into such composition. 2. The process of claim 1 , where the base used in step i) is selected from metal hydroxides.3. The process of claim 1 , where Ris methyl.4. The process of claim 1 , where the alcohol R—OH is selected from methanol claim 1 , ethanol or isopropanol.5. The process of claim 1 , where the reacting step i) is performed at a temperature in a range of from −10 to 50° C.6. The process of claim 1 , where the reaction product mixture of the step i) is directly applied in step ii).7. The process of claim 1 , where the hydrogenation catalyst comprises at least one metal selected from the group consisting of nickel claim 1 , rhodium and palladium.8. The process of claim 1 , further comprising distilling a reaction mixture obtained in the step iii).9. The process of claim 1 , where the steps i) and ii) or the step iii) claim 1 , or all steps i) to iii) claim 1 , are performed in a continuous manner.11. The compound according to claim 10 , where Ris methyl and Ris C-C-alkyl.12. The compound 5-methoxy-1-(2 claim 10 ,6 claim 10 ,6-trimethylhexen-1-yl)hex-1-en-3-one.13. (canceled)14. A fragrance or a flavor composition comprising{'claim-ref': {'@idref': 'CLM-00010', 'claim 10'}, 'a) at least one compound (I.a), as defined in ,'}b) optionally at least one aroma chemical different from the compounds (I.a), andc) optionally at least one carrier,with the proviso that the composition comprises at least one of the components b) ...

Nitric oxide donors

The present invention provides, in part a novel class of nonoate compounds which exhibit nitric oxide releasing activity and their pharmaceutically acceptable salts, esters and prodrugs. The compounds release nitric oxide upon activation by contact with plasma. The present invention also relates to the use of the disclosed compounds to deliver nitric oxide to treat disorders arising from nitric oxide dysregulation.

COMPOSITIONS AND METHODS FOR THE DELIVERY OF NUCLEIC ACIDS

A nanosized complex includes a nucleic acid and a compound comprising formula (I): 3. The complex of claim 1 , wherein Rand Rare independently a hydrophobic group derived from oleic acid or linoleic acid.4. The complex of claim 3 , wherein Rand Rare the same.5. The complex of claim 1 , wherein at least one of Ror Rincludes all-trans-retinylamine or (1R)-3-amino-1-[3-(cyclohexylmethoxy)phenyl]propan-1-ol.6. The complex of claim 1 , wherein a claim 1 , b claim 1 , c claim 1 , and d are each 2.7. The complex of claim 1 , Rcomprises at least one of CHCHNH claim 1 , CHCHNHCHCHNHCHCHNH claim 1 , or CHCHNHCHCHCHCHNHCHCHCHNH.8. The complex of claim 1 , wherein the retinoid or retinoid derivative is covalently attached to a thiol group of a cysteine residue by a linker.9. The complex of claim 8 , wherein the linker comprises a polyamino acid group claim 8 , a polyalkylene group claim 8 , or a polyethylene glycol group.10. The complex of claim 8 , wherein the linker comprises an acid labile bond.11. The complex of claim 1 , wherein the nucleic acid is capable of treating claim 1 , ameliorating claim 1 , attenuating claim 1 , and/or eliminating symptoms of a disease or disorder of the eye when the complex is introduced to or within the eye of a subject with a disease or disorder.12. The complex of claim 11 , wherein the nucleic acid comprises a siRNA or plasmid DNA.13. The complex of claim 10 , wherein the nucleic acid includes plasmid DNA encoding at least one of an ATP-binding cassette transporter claim 10 , RPE65 claim 10 , RHO claim 10 , RdCVF claim 10 , or CP290.15. The method of claim 14 , wherein Rand Rare independently a hydrophobic group derived from oleic acid or linoleic acid.16. The method of claim 14 , wherein at least one of Ror Rincludes all-trans-retinylamine or (1R)-3-amino-1-[3-(cyclohexylmethoxy)phenyl]propan-1-ol.17. The method of claim 14 , Rcomprises at least one of CHCHNH claim 14 , CHCHNHCHCHNHCHCHNH claim 14 , or CHCHNHCHCHCHCHNHCHCHCHNH.18. The method ...

METHOD FOR SYNTHESIS OF 9-CIS-BETA-CAROTENE AND FORMULATIONS THEREOF

The present invention relates to a method for total chemical synthesis of 9-cis-β-carotene (9CBC), and further provides stable formulations thereof. 2. The formulation of claim 1 , wherein said thickening/solidifying agent comprises a lecithin or a PEGylated derivative thereof; a lecithin-like substance; a medium chain triglyceride or a mixture thereof; a povidone; a polysorbate; or sorbitol.3. The formulation of claim 2 , wherein said thickening/solidifying agent comprises a lecithin or a PEGylated derivative thereof claim 2 , a lecithin-based product claim 2 , or a povidone.4. The formulation of claim 3 , wherein said lecithin is egg lecithin or soybean lecithin; or said lecithin-based product is L-α-lecithin claim 3 , granular (Acros Organics™) claim 3 , Phospholipon® 50 claim 3 , Phospholipon® 75 claim 3 , Phospholipon® 85G claim 3 , Phospholipon® 90G claim 3 , Phospholipon® 80H claim 3 , Phospholipon® 90H claim 3 , Phospholipon® E25 claim 3 , Phospholipon® E35 claim 3 , Phospholipon® E claim 3 , Phospholipon® LPC20 claim 3 , Phospholipon® LPC25 claim 3 , or Phospholipon® LPC65.5. The formulation of claim 2 , wherein said lecithin-like substance is egg yolk; said medium chain triglyceride is miglyol claim 2 , miglyol 810 claim 2 , or a mixture thereof; or said polysorbate is polysorbate 20 claim 2 , polysorbate 40 claim 2 , polysorbate 60 claim 2 , or polysorbate 80.6. The formulation of claim 1 , wherein said antioxidant is a thiol; a sulphoximine; a metal chelator; sodium bisulfite; sodium metabisulfite; a vitamin; a phenol; a benzoate; uric acid; mannose; propyl gallate; a selenium; a stilbene; a carotenoid; or a mixture thereof.7. The formulation of claim 6 , wherein said antioxidant is a phenol selected from the group consisting of BHT claim 6 , butylhydroxyanisole claim 6 , ubiquinol claim 6 , nordihydroguaiaretic acid claim 6 , and trihydroxybutyrophenone; a carotenoid selected from the group consisting of α-carotene claim 6 , β-carotene claim 6 , β- ...

Compounds for the treatment of hiv

The invention provides compounds of formula (I): or a salt thereof as described herein. The invention also provides pharmaceutical compositions comprising a compound of formula (I), processes for preparing compounds of formula (I), intermediates useful for preparing compounds of formula I and therapeutic methods for treating a Retroviridae viral infection including an infection caused by the HIV virus.

叶黄素的转化方法

一种用碱－催化异构化把自然界存在的叶黄素或其酯转化成玉米黄质的方法。该方法包括在高于约50℃下加热在碱金属氢氧化物水溶液与二甲基亚砜或与饱和烷烃和/或芳烃有机溶剂的混合物中的已经或未经预处理过的含叶黄素的天然产物或纯叶黄素,当采用烃类为有机溶剂时,该方法在相转移催化剂存在下进行。玉米黄质具有许多用途。特别用于做色料。

Method For Extraction and Concentration of Carotenoids Using Supercritical Fluids

Carotenoids are extracted and/or enriched from a mixture containing such compounds. The extraction/enrichment process involves the use of liquefied or supercritical solvents to extract lipids and carotenoids from carotenoid-containing substrates. The extraction process can also be performed in two steps in which lipids and carotenoids are first removed from a carotenoid-containing substrate with a liquefied or supercritical solvent, and subsequently a liquefied or supercritical gas is used to separate the lipids from the carotenoids. The two step process can be reversed to first extract lipids with the liquefied or supercritical gas, and subsequently use the solvent to extract the carotenoids. The process is also applicable to yield an organic solvent-free product from a carotenoid-containing source that was first extracted using an organic solvent.

Recovery of carotenoids, tocopherols, tocotrienols and sterols from esterified palm oil

The invention is for a method for the isolation of the minor non-glyceride components of palm oil or like vegetable oil containing free fatty acid and non-glyceride components similar to that of palm oil which method comprises: (i) esterifying the free fatty acid component of the oil with one or more monohydric alcohols to form an esterified oil with every low free fatty acid content, (ii) converting the glycerides into monoesters by transesterification employing one or more monohydric alcohols, (iii) adsorbing the non-glyceride components onto a selective absorbent to separate said components from the esters of the oil, and (iv) thereafter desorbing the non-glyceride components from the adsorbent with the use of solvent to recover said components. The adsorbent is preferably activated alumina, activated carbon, or silica gel, preferably reverse phase (particularly C18) silica gel. By the method, carotenes, sterols, tocopherols and other non-glyceride components can be isolated.

Method for producing solutions of astaxanthin derivatives

Formulation of astaxanthin derivatives and use thereof iii

虾青素衍生物的配制剂及其应用i

本发明涉及虾青素衍生物的配制剂，其呈虾青素衍生物在适合食品的有机溶剂中的溶液形式，其中有机溶剂选自油、脂肪和蜡及其混合物，所述配制剂的虾青素衍生物含量相对于所述配制剂的总重量大于2重量％，其中虾青素衍生物包含至少80重量％，特别是至少90重量％，尤其是至少96重量％的至少一种式I化合物，其中全反式异构体(I-反式)的比例相对于所述溶液中所含式(I)化合物的总量小于80重量％，特别是至多75重量％，尤其是至多70重量％，特别是40％至＜80％，优选45-75％，尤其是50-70％。虾青素衍生物为下式(I)的化合物，其中R为式(R)的基团，其中#表示与羰基的链接，A为-CH 2 CH 2 -或-CH＝CH-且R x 为C 1 -C 4 烷基；并且虾青素衍生物为包含至少80重量％，特别是至少90重量％，尤其是至少96重量％式(I)化合物的虾青素衍生物。

虾青素衍生物的粉状组合物ii

本发明涉及由下列成分组成的粉状组合物：i)相对于该组合物的总重量为1-50重量％的虾青素衍生物，该衍生物的至少70重量％由下面所定义的式(I)化合物构成，ii)相对于该组合物的总重量为至少10重量％至70重量％的至少一种蛋白质保护性胶体，和iii)任选地，相对于该组合物的总重量为至多89重量％的一种或多种适合食物的添加剂。在式(I)中，R为下式的基团，其中#表示与羰基的链接，A为-CH 2 CH 2 -或-CH＝CH-且R x 为C 1 -C 4 烷基。

Formulierung von astaxanthin-derivaten und deren verwendung i

Die vorliegende Erfindung betrifft Formulierungen von Astaxanthin-Derivaten in Form einer Lösung des Astaxanthinderivats in einem für Nahrungsmittel geeigneten organischen Lösungsmittel, das unter Ölen, Fetten und Wachsen und deren Gemischen ausgewählt ist, mit einem Gehalt an Astaxanthinderivat von mehr als 2 Gew.-%, bezogen auf das Gesamtgewicht der Formulierung, wobei das Astaxanthin-Derivat zu wenigstens 80 Gew.-%, insbesondere wenigstens 90 Gew.-% und speziell zu wenigstens 96 Gew.-% aus wenigstens einer Verbindung der Formel (I) besteht, wobei der Anteil des all-trans-lsomeren (l-trans), bezogen auf die Gesamtmenge der in der Lösung enthaltenen Verbindung der Formel (I), weniger als 80 %, insbesondere höchstens 75 Gew.-% und speziell höchsten 70 Gew.-%, insbesondere im Bereich von 40 % bis < 80 %, bevorzugt im Bereich von 45 % bis 75 % und speziell im Bereich von 50 bis 70 % liegt. Bei den Astaxanthin-Derivaten handelt es sich um Verbindungen der folgenden Formel (I) worin R für einen Rest der Formel (R) steht, worin # die Anknüpfung an die Carbonylgruppe bedeutet, A für -CH2CH2- oder für -CH=CH- steht und Rx für C1-C4 Alkyl steht; sowie um Astaxanthin-Derivate, die zu wenigstens 80 Gew.-%, insbesondere wenigstens 90 Gew.-% und speziell zu wenigstens 96 Gew.-% aus den Verbindungen der Formel (I) bestehen.

Formulation of astaxanthin derivatives and use thereof iii

The invention relates to formulations of an astaxanthin derivative, comprising a continuous oil phase with at least one oil that is suitable for foodstuffs and an aqueous phase that is emulsified in the oil phase, the astaxanthin derivative being present in the aqueous phase in the form of dispersed particles that are stabilised by at least one protective colloid. The astaxanthin derivative consists of at least 70 % by weight, preferably at least 80 % by weight, in particular at least 90 % by weight and especially 96 % by weight of a compound of formula (I) below. In formula (I), R represents a group of formula (III), where # is the link to the carbonyl group, A represents -CH 2 CH 2 - or -CH=CH- and R x represents C 1 -C 4 alkyl.

Verfahren zur herstellung von lösungen von astaxanthin-derivaten

Die vorliegende Erfindung betrifft ein Verfahren zur Herstellung einer Lösung eines Astaxanthin-Derivats in einem für Nahrungsmittel geeigneten Öl, umfassend die folgenden Schritte: i) Bereitstellen einer Suspension oder Lösung des Astaxanthin-Derivats in einem organischen, aus Sauerstoff, Wasserstoff und Kohlenstoff bestehenden, für Nahrungsmittel geeigneten Lösungsmittel, das unter C 2 -C 6 -Alkanolen, C 1 -C 4 -Alkylestern aliphatischer C 1 -C 4 -Carbonsäuren und aliphatischen Ketonen mit 3 bis 6 C-Atomen ausgewählt ist, ii) Einarbeiten der Lösung oder Suspension des Astaxanthin-Derivats in ein für Nahrungsmittel geeignetes Öl, wobei man eine Lösung des Astaxanthin-Derivats erhält; wobei das Astaxanthin-Derivat zu wenigstens 70 Gew.-%, bevorzugt zu wenigstens 80 Gew.-%, insbesondere zu wenigstens 90 Gew.-% und speziell zu wenigstens 96 Gew.-% aus wenigstens einer Verbindung der Formel (I) besteht. Formel (I), worin R für einen Rest der Formel (II) steht, worin # die Anknüpfung an die Carbonylgruppe bedeutet, A für -CH 2 CH 2 - oder für -CH=CH- steht und R x für C 1 -C 4 Alkyl steht.

Pulverförmige zusammensetzungen von astaxanthin-derivaten ii

Die vorliegende Erfindung betrifft pulverförmige Zusammensetzungen, welche aus den folgenden Bestandteilen besteht: i) einem Astaxanthin-Derivat, das zu wenigstens 70 Gew.-% aus einer Verbindung der im folgenden definierten Formel (I) besteht, in einer Menge von 1 bis 50 Gew.- %, bezogen auf das Gesamtgewicht der Zusammensetzung, ii) wenigstens einem proteinischen Schutzkolloid in einer Menge von wenigstens 10 bis 70 Gew.-%, bezogen auf das Gesamtgewicht der Zusammensetzung, und iii) gegebenenfalls einem oder mehreren, für Nahrungsmittel geeigneten Zusatzstoffen in einer Menge von bis zu 89 Gew.-%, bezogen auf das Gesamtgewicht der Zusammensetzung. In Formel (I) steht R für einen Rest der Formel worin # die Anknüpfung an die Carbonylgruppe bedeutet, A für -CH 2 CH 2 - oder für -CH=CH- steht und R x für C 1 -C 4 Alkyl steht.

生产虾青素衍生物的溶液的方法

本发明涉及一种生产虾青素衍生物在适合食物的油中的溶液的方法，所述方法包括下列步骤：i)提供虾青素衍生物在适合食物的有机溶剂中的悬浮液或溶液，所述有机溶剂由氧、氢和碳构成且选自C 2 -C 6 链烷醇、脂族C 1 -C 4 羧酸的C 1 -C 4 烷基酯和具有3-6个碳原子的脂族酮；ii)将所述虾青素衍生物的溶液或悬浮液掺入适合食物的油中，由此得到虾青素衍生物溶液。虾青素衍生物包含至少70重量％，优选至少80重量％，特别是至少90重量％，尤其是至少96重量％的式(I)化合物，其中R为式(II)的基团，其中#表示与羰基的链接，A为-CH 2 CH 2 -或-CH＝CH-且R x 为C 1 -C 4 烷基。

Formulation of astaxanthin derivatives and use thereof

Dimer poly-quaternary ester compounds

The present invention relates to a novel class of polymeric compounds having specific quaternized amine based upon a dimer acid reacted with an alkanolamine to make an ester quaternary compound. Dimer acid is a C-36 diacid having a cyclic structure and two amine groups that allow for the synthesis of a high molecular weight cationic compound which is extremely substantitive to human skin and are well tolerated by human tissue making them suitable for use preparation of barrier products for personal care applications. These materials are dimethylaminopropyl amine free, which is highly desirable in personal care applications.

Processo para a produ-Æo de ironas

Process for the catalytic reduction of alkyne compounds

Asymmetric synthesis and catalysis with chiral heterocyclic compounds

This invention relates to chiral heterocyclic compounds useful for asymmetric synthesis and catalysis. More particularly, the invention relates to chiral heterocyclic phosphine, sulfur, and nitrogen compounds for asymmetric synthesis and catalysis in the production of enantiomerically pure products.

Asymmetric synthesis and catalysis with chiral heterocyclic compounds

This invention relates to chiral heterocyclic compounds useful for asymmetric synthesis and catalysis. More particularly, the invention relates to chiral heterocyclic phosphine, sulfur, and nitrogen compounds for asymmetric synthesis and catalysis in the production of enantiomerically pure products.

Process for the production of beta-carotene preparations with a high 9 (Z) content

Catalytic hydrogenation of alpha,beta-unsaturated aldehydes to alpha,beta-unsaturated alcohols

Improved, selective hydrogenation of alpha, beta-unsaturated aldehydes to alpha,beta-unsaturated alcohols utilizing a platinum-cobalt catalyst.

Method of preparing sulfones

Method for extraction of carotene from carotene-containing materials

FIELD: chemical technology. SUBSTANCE: invention relates to extraction of carotenes from carotene-containing materials. Method for extraction of carotenes from carotene-containing material, in particular, fats and oils of biological origin provides extraction of indicated carotene-containing materials with extractant comprising at least one component taken among the group including acetonitrile, N-methylpyrrolidone, N,N-dimethylformamide, N, N-dimethylacetamide, 4-formylmorpholine, 4-acetylmorpholine, 4-methylformalin, 4-phenylmorpholine to form two liquid phase. One phase is carotene-depleted residue phase and another phase is carotene-enriched phase followed by separation of two liquid phases. Invention provides increasing yield of carotenes in carrying out the direct extraction procedure. EFFECT: improved extraction method. 15 cl, 8 ex СОУС сСс ПЧ сэ (19) РОССИЙСКОЕ — АГЕНТСТВО ПО ПАТЕНТАМ И ТОВАРНЫМ ЗНАКАМ КО (51) МПК? (11) (13) 2 224 012 С2 С 11 В 1/10, С 09 В 61/00 12 ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ РОССИЙСКОЙ ФЕДЕРАЦИИ (21), (22) Заявка: 2000131224/13 , 11.05.1999 (24) Дата начала действия патента: 11.05.1999 (30) Приоритет: 11.05.1998 ОЕ — 19821009.4 (46) Дата публикации: 20.02.2004 (56) Ссылки: Ч$ 5714658 А, 03.02.1998. СВ 1562794 А, 19.03.1980. КУ 1608901 С1, 20.01.1995. ЕР 0670306 А, 06.09.1995. М/О 9629306 А, 26.09.1996. ЕР 0242148 А, 21.10.1987. УМО 9803480 А, 29.01.1998. (85) Дата перевода заявки РСТ на национальную фазу: 13.12.2000 (86) Заявка РСТ: ЕР 99/03219 (11.05.1999) (87) Публикация РСТ: Мо 99/58611 (18.11.1999) (98) Адрес для переписки: 190000, Санкт-Петербург, наб.Мойки, 58, Патентика, пат.пов.М.И.Ниловой, рег.№378 (72) Изобретатель: ДРЕШЕР Мартин (ОЕ), ВАИДНЕР Эхард (0Е), ПЕТЕР Зигфрид (РЕ) (73) Патентообладатель: ПЕТЕР Зигфрид (0Е) (74) Патентный поверенный: Нилова Мария Иннокентьевна (54) СПОСОБ ИЗВЛЕЧЕНИЯ КАРОТИНА ИЗ КАРОТИНОСОДЕРЖАЩИХ МАТЕРИАЛОВ (57) Изобретение относится к способу извлечения каротинов из каротиносодержащих материалов. ...

生产鸢尾酮的方法

本发明描述了一种通过鸢尾酮前体的化学氧化制备鸢尾酮的方法，包括处理从下列组中选出的鸢尾根状茎底物：鸢尾根状茎、这种根状茎的部分、鸢尾提取物、鸢尾提取物废物、任何含有鸢尾酮前体或其混合物的植物组织。

一种维生素a中间体双格氏缩合物的连续水解中和的方法及装置

本发明公开了一种维生素A中间体双格氏缩合物的连续水解中和的方法及装置。步骤为，将含有维生素A中间体双格氏缩合物的醚类溶液与酸水分别泵入管式反应器，经管式反应器充分混合进行连续水解得到水解液；碱水经管式反应器另一进料口泵入管式反应器，与所述水解液在管式反应器中进行连续中和得到中和液；所述中和液从管式反应器的产物排出口排出，分层成水相和有机相，除去所述水相，所述有机相水洗至中性后，蒸发回收有机溶剂，得到维生素A中间体缩合物。采用本发明的方法混合效率高，时间短，产物的纯度和收率高；含量高，折纯收率高。同时可实现连续化操作，安全可靠，改善生产作业人员的工作环境，提高生产效率和设备利用率。

虾青素酯

通式(I)的虾青素衍生物，式中R每种情况是基团－NH－CH(R 1 )－COOR 2 (a)、OR 3 (b)或－(Y)n－Z(c)，而R 1 、R 2 、R 3 、Y、Z及n如说明书中表示的详细含义，是一类新颖的化合物，它们在饲料制造所要求的高温挤出中以及在制造出的饲料的贮存期间具有高的稳定性，因此它们适用作为水生动物饲料的着色类胡萝卜素。这些衍生物的制备方法是：虾青素与合适的酸RCOOH本身或其酰氯(RCOCl)或其酸酐(RCO) 2 O起反应，或者在R表示(a)基团的情况下，虾青素与通式为OCNCH(R 1 )COOR 2 的合适N－羰基－氨基酸酯起反应。本发明还涉及含有这种虾青素衍生物作为着色用类胡萝卜素的水生动物饲料的配料，和涉及生产这种配料的方法，此生产方法是：将虾青素衍生物溶于植物的或蔬菜的油或脂中，或溶于有机溶剂中，或溶于植物的或蔬菜的油或脂与有机溶剂的混合物中；将此溶液用保护胶体的水溶液进行乳化；至少部分除去溶剂和水，得到浓乳化液；以及将此浓乳化液喷雾干燥以便最终生成适合于加至水生动物饲料的配料中。本发明还涉及含有这种着色用类胡萝卜素的水生动物饲料。

类胡萝卜素衍生物、其药学上可接受的盐或者其药学上可接受的酯类或酰胺类

本发明的课题在于发现一种水溶性优异的类胡萝卜素化合物。其为具有通式(I)[式中，X表示羰基或亚甲基，R 1 和R 2 为(a)或(b)，剩余的为(a)、(b)、(c)或氢原子，(a)－CO－A－B－D{式中，A为亚烷基、亚烯基等，B为式－S(O)n－、式－NR 4 CONR 5 －，D为氢原子、羧基等}；(b)：－CO－E－F{式中，E表示亚烷基、式－NR 3 －(式中，R 3 表示(a1)氢原子、(b1)烷基等)，F表示磺基}；(c)：－CO－G{式中，G表示氢原子、烷基等}]的类胡萝卜素衍生物、其药学上可接受的盐或者其药学上可接受的酯类或酰胺类。

Crystalline form of compound suppressing protein kinase activity and the use thereof

FIELD: chemical engineering. SUBSTANCE: invention relates to a compound represented by the structural formula (I) ({5-[(1R)-1-(2,6-dichloro-3-fluorophenyl)ethoxy]-6-aminopyridazin -3-yl}-N-{4-[((3S,5R)-3,5-dimethylpiperazinyl)carbonyl]phenyl}carboxamide hydrochloride) and its novel crystalline form of a dihydrate and a trihydrate as well as a method for producing a compound and a crystalline form corresponding to intermediate compounds, a pharmaceutical composition containing a compound according to the invention, use for preparing a pharmaceutical product for the treatment of a disease, disorder or condition in a patient where the disease, disorder or condition is associated with c-Met, CSF1R, ROS1 or a fused protein based on ROS1, TRKA or a fused protein based on TRKA, TRKB, TRKC, ALK, ALK ATI or a fused protein based on ALK. EFFECT: technical result: obtained are novel crystalline forms of the compound of formula (I) showing better solubility and higher suction. 35 cl, 12 dwg, 32 tbl, 14 ex РОССИЙСКАЯ ФЕДЕРАЦИЯ ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) (19) RU (11) (13) 2 744 264 C2 (51) МПК C07D 403/10 (2006.01) C07D 403/12 (2006.01) A61K 31/501 (2006.01) A61P 3/00 (2006.01) A61P 9/00 (2006.01) A61P 25/00 (2006.01) A61P 35/00 (2006.01) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ (52) СПК C07C 403/10 (2020.08); C07D 403/12 (2020.08); A61K 31/501 (2020.08); A61P 3/00 (2020.08); A61P 9/00 (2020.08); A61P 25/00 (2020.08); A61P 35/00 (2020.08) (21)(22) Заявка: 2018145183, 01.06.2017 01.06.2017 Дата регистрации: (73) Патентообладатель(и): ЭксКАВЕРИ ХОЛДИНГЗ, ИНК. (US) 04.03.2021 01.06.2016 CN PCT/CN2016/084300 (43) Дата публикации заявки: 14.07.2020 Бюл. № 20 (45) Опубликовано: 04.03.2021 Бюл. № 7 (86) Заявка PCT: CN 2017/086760 (01.06.2017) C 2 C 2 (85) Дата начала рассмотрения заявки PCT на национальной фазе: 09.01.2019 (56) Список документов, цитированных в отчете о поиске: WO 2012048259 A2, 12.04.2012. Mino R. Caira, Crystalline Polymorphism of Organic ...

Method of extracting lutein/xanthophylls from natural materials and highly purified lutein/xanthophylls obtained from the method thereof

본 발명은 천연 재료들로부터 루테인을 추출하는 새로운 방법을 제공하며 천연 재료들에 있는 천연 루테인 에스터의 유리 루테인 및/또는 저 분자량 루테인 에스터로의 변형, 최적 조건에서 초임계 유체에 의한 상기 천연 재료들의 추출을 포함한다. 상기 방법은 추출에 사용된 온화한 조건 때문에 고순도의 다량의 미정제 루테인을 생산하다. 따라서, 원하는 생성물의 열화가 일어나지 않는다. 미정제 루테인은 고순도 루테인을 얻기 위해 크로마토그래피에 의해 추가로 정제될 수 있다. 본 발명에 따른 방법은 잔토필 또는 루테인 이외의 다른 것의 추출에 적용될 수 있다. The present invention provides a novel method of extracting lutein from natural materials and includes the conversion of natural lutein esters into free lutein and / or low molecular weight lutein esters in natural materials, Extraction. The process produces large amounts of crude lutein of high purity due to the mild conditions used in the extraction. Therefore, deterioration of the desired product does not occur. The crude lutein can be further purified by chromatography to obtain high purity lutein. The method according to the present invention can be applied to the extraction of other than xanthophyll or lutein.

베타-카로틴의 효율적인 제조방법

본 발명은 설폰 화학을 이용하여 카로틴 화합물의 합성에 유용하게 이용되는 신규의 중간체 화합물, 그 제조방법, 및 상기 중간체 화합물을 이용한 베타-카로틴의 효율적인 제조방법을 제공한다. 베타-카로틴의 제조방법은 탄소 10개로 이루어진 상기 중간체 화합물의 양끝에 있는 두 알데하이드 작용기에 각각 C 15 알릴릭 설폰 화합물을 반응시켜 탄소 40개로 이루어진 알코올 화합물을 얻고, 상기 C 40 화합물의 두 알코올기를 할로겐 또는 에테르로 변형시킨 다음, 더블 엘리미네이션(double elimination)의 방법으로 설폰기와 할로겐(또는 에테르)기를 모두 제거하며 이중결합을 형성하는 방법으로 컨쥬게이트 폴리엔 사슬 구조를 형성한 데 그 특징이 있다. 베타-카로틴, 설폰 화합물, 알데하이드, 폴리엔 체인, 더블 엘리미네이션

一种c15砜的制备方法

本发明公开了C15砜的制备方法，解决了生产过程中的环保问题，其技术方案要点是采用苯亚磺酸替代苯亚磺酸盐为原料，采用水替代醋酸为反应介质，采用间歇或连续式微波反应器，能够大幅提高反应效率降低反应时间，提高原料转化率和产品收率。反应生成产物和水，水可以回用不产生废水，工艺绿色环保。同时本公开采用的微波反应器的内腔壁设有向箱体内部方向的凸槽，可以使反应器吸收微波更为均匀。整体工艺流程简单，反应条件温和，安全环保，易于实现产品的连续化、规模化生产。

一种水溶性叶黄素的绿色制备方法

一种水溶性叶黄素的绿色制备方法，涉及一种叶黄素由油溶性改性为水溶性的工艺技术，属于营养补充剂、天然食品着色剂领域。主要通过叶黄素与甜菊苷分子非共价结合、特定方法和条件的改性，制备得到水溶性叶黄素的溶解度增加150倍以上，且稳定性好；通过低频超声、高压剪切与天然抗氧化剂使用等，避免了叶黄素的异构与降解，使产品中反式叶黄素比例大于85％；可制备成多种剂型或添加入水溶性溶媒、多种功能食品中，发挥叶黄素的生物活性。本发明方法未使用乳化剂、表面活性剂等辅料，制备过程无有害溶剂残留，具有工艺条件绿色、原料天然等特点。

Retinoic acid derivative, process for preparing the same, and cosmetic composition comprising the same

PURPOSE: A retinoic acid derivative is provided to have low cytotoxicity, and a collagen synthetic activity, thereby improving wrinkle-reducing effect of a cosmetic composition. CONSTITUTION: A manufacturing method of retinoic acid derivative indicated in chemical formula 1 comprises: a step of synthesizing -Gly-Arg-Glu-Pro by reacting Fmoc-amino acid onto an aminomethyl polystyrene or 2- chlorotrityl chloride polystyrene resin in which a rink amide is accepted under the presence of a coupling agent, and removing Fmoc by treating the result by 20% piperidine/NMP; a step of combining retinoic acid to the -Gly-Arg-Glu-Pro; a step of treating the result by 25% trifluoroacetic acid and dichloromethane to separate the compound indicated in chemical formula 1 from the solid resin. In chemical formula 1, R is -Gly-Arg-Glu-Pro-NH2.

一种快速制备高含量叶黄素的工业化方法及其制品

本发明涉及一种快速制备高含量叶黄素的工业化方法及其制品，包括如下步骤：1)在高温下用体积分数为90～100％的丙酮溶液对万寿菊花颗粒进行提取；2)将提取液在低温下静置，至高含量的叶黄素完全析出，即得。本发明发现，体积分数为90～100％的丙酮溶液对万寿菊花颗粒中的叶黄素的提取有非常高的选择性，且随温度的变化叶黄素在上述溶液中的溶解度有明显的变化，可实现对叶黄素进行高含量、高得率提取，提取得到的产品中叶黄素的含量提高到50％。与经典工艺正己烷/石油醚提取和浓缩得到叶黄素浸膏相比，含量提高了约2倍。

Carotenoid derivative, its pharmaceutically acceptable salt and pharmaceutical composition containing it

FIELD: chemistry. SUBSTANCE: present invention relates to a carotenoid derivative of general formula (I), or a pharmaceutically acceptable salt thereof, having anti-inflammatory activity, as well as to containing as an active ingredient a carotenoid derivative of general formula (I), or its pharmaceutically acceptable salt of pharmaceutical composition . In formula (I) X is a carbonyl group or a methylene group, R 1 and R 2 in general formula (I) are one and same or different and each represents -CO-ABD; A, B and D have values given in the claim. EFFECT: carotenoid derivative, its pharmaceutically acceptable salt and pharmaceutical composition containing it are disclosed. 11 cl, 4 dwg, 46 tbl, 42 ex РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (51) МПК C07C 403/24 (2006.01) A61K 31/27 (2006.01) A61P 3/04 (2006.01) A61P 3/06 (2006.01) A61P 9/04 (2006.01) A61P 9/12 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА A61P 21/00 (2006.01) ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ A61P 25/18 (2006.01) A61P 25/24 (2006.01) A61P 25/28 (2006.01) (12) (13) 2 693 455 A61P 27/00 A61P 27/02 A61P 27/06 A61P 29/00 A61P 35/00 C2 (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ (52) СПК (21)(22) Заявка: 2016149777, 20.05.2015 (24) Дата начала отсчета срока действия патента: Дата регистрации: 03.07.2019 (73) Патентообладатель(и): Аста Фармасьютикалз Ко., Лтд. (JP) Приоритет(ы): (30) Конвенционный приоритет: 20.05.2014 JP 2014-104480; 08.12.2014 JP 2014-247549 (56) Список документов, цитированных в отчете о поиске: JP 2013518856 А, 23.05.2013. JP (45) Опубликовано: 03.07.2019 Бюл. № 19 2 6 9 3 4 5 5 (86) Заявка PCT: R U (85) Дата начала рассмотрения заявки PCT на национальной фазе: 20.12.2016 2010248243 A, 04.11.2010. JP 2007176814 A, 12.07.2007. JP 2006517197 А, 20.07.2006. JP 2005517010 А, 09.06.2005. RU 2005125072 A, 10.06.2006. (54) КАРОТЕНОИДНОЕ ПРОИЗВОДНОЕ, ЕГО ФАРМАЦЕВТИЧЕСКИ ПРИЕМЛЕМАЯ СОЛЬ И ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ, СОДЕРЖАЩАЯ ЕГО (57) Реферат: Настоящее изобретение относится к ...

The method of obtaining-carotene

纯化虾青素的方法

本发明涉及制造二氯甲烷含量≤250ppm的合成的食品级虾青素的方法，所述方法包括以下步骤：a)在反应器中提供含二氯甲烷的合成的虾青素晶体；和b)向合成的虾青素晶体中加入一定量的甲醇以获得合成的虾青素在甲醇中的悬浮物，其中基于悬浮物的总重量，所述悬浮物中合成的虾青素的量在5‑70重量％的范围内，并关闭所述反应器；和c)使在步骤b)中获得的悬浮物达到80‑140℃范围内的温度；和d)使悬浮物维持在于步骤c)中所达到的温度下；和e)通过释放超压使合成的虾青素的甲醇悬浮物达到大气压；和f)将合成的虾青素悬浮物冷却至10‑35℃范围内的温度；和g)滤出合成的虾青素晶体并干燥；其中在所述方法期间，合成的虾青素的总量未同时完全溶解在甲醇中，且其中获得了二氯甲烷含量＜250ppm的合成的食品级虾青素。还可以使用合成的AXN在二氯甲烷中的溶液代替合成的虾青素晶体作为起始材料。

制造9－顺式视黄酸的方法

描述了一种新的可工业化应用的制造9－(Z)－视黄酸的方法，其特征在于3－甲基－4－氧代巴豆酸的碱金属盐和C 15 －三苯基鏻盐的转化。9－(Z)－视黄酸是用于治疗多种皮肤病的多用途化合物。